Journal articles: 'Biological Active Molecules'

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Freeman, Amihay, Yael Dror, Carmit Ophir Porat, Noa Hadar, and Yossi Shacham Diamand. "Silver-Coated Biologically Active Protein Hybrids: Antimicrobial Applications." Applied Mechanics and Materials 749 (April 2015): 453–56. http://dx.doi.org/10.4028/www.scientific.net/amm.749.453.

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Novel hybrids, comprised of a biologically active protein molecule core, coated with a thin outer layer of porous metallic silver, were developed in our lab. By the conjugation of silver reducing polymer to the surface of soluble, molecular, biologically active protein molecules and subsequent addition of silver salt, electroless silver deposition, culminating in thin porous metallic coating, was directed to the surface of the protein molecules. The silver-protein hybrids thus obtained, presenting novel nanoparticles several nanometers in size, retained their solubility and biological activity.The silver coating combined with the retained biological activity of its protein core, paved the way to a series of biomedical applications of these hybrids including "wiring" of the active site of oxido-reductase enzyme to electrodes, imaging of the presence of targeted ligands displayed on cancer cell surface and antimicrobial enzymatically attenuated release of silver ions.In this presentation we shall overview the technology of protein-silver hybrid's fabrication and analytical applications of silver-glucose oxidase and silver-Avidin hybrids, followed by feasibility demonstration of using silver-glucose oxidase hybrid as novel antibacterial and antifungal agent.

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Rana, Aniruddhasinh M., Kishor R. Desai, and Smita Jauhari. "Rhodanine-based biologically active molecules: synthesis, characterization, and biological evaluation." Research on Chemical Intermediates 40, no. 2 (January 22, 2013): 761–77. http://dx.doi.org/10.1007/s11164-012-1001-3.

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Insuasty, Daniel, Juan Castillo, Diana Becerra, Hugo Rojas, and Rodrigo Abonia. "Synthesis of Biologically Active Molecules through Multicomponent Reactions." Molecules 25, no. 3 (January 24, 2020): 505. http://dx.doi.org/10.3390/molecules25030505.

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Focusing on the literature progress since 2002, the present review explores the highly significant role that multicomponent reactions (MCRs) have played as a very important tool for expedite synthesis of a vast number of organic molecules, but also, highlights the fact that many of such molecules are biologically active or at least have been submitted to any biological screen. The selected papers covered in this review must meet two mandatory requirements: (1) the reported products should be obtained via a multicomponent reaction; (2) the reported products should be biologically actives or at least tested for any biological property. Given the diversity of synthetic approaches utilized in MCRs, the highly diverse nature of the biological activities evaluated for the synthesized compounds, and considering their huge structural variability, much of the reported data are organized into concise schemes and tables to facilitate comparison, and to underscore the key points of this review.

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Karolak-Wojciechowska, J., and A. Fruzinski. "Spacer conformation in biologically active molecules." Pure and Applied Chemistry 76, no. 5 (January 1, 2004): 959–64. http://dx.doi.org/10.1351/pac200476050959.

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Based on our contemporary studies on the structures of biologically active molecules, we focus our attention on the aliphatic chain and its conformation. That flexible spacer definitely influenced the balanced position of all pharmacophoric points in molecules of biological ligands. The one atomic linker and two or three atomic spacers with one heteroatom X =O, S, CH2, NH have been taken into account. The conformational preferences clearly depend on the heteroatom X. In the discussion, we utilize our own X-ray data, computation chemistry methods, population analysis, and statistical data from the Cambridge Structural Database (CSD).

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LIU, Yan, and Rong GUO. "Interaction between organized assemblies of amphiphilic molecules and biological active molecules." Chinese Science Bulletin 62, no. 6 (November 14, 2016): 486–97. http://dx.doi.org/10.1360/n972016-00426.

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Smith, David P. "Active learning in the lecture theatre using 3D printed objects." F1000Research 5 (June 3, 2016): 61. http://dx.doi.org/10.12688/f1000research.7632.2.

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The ability to conceptualize 3D shapes is central to understanding biological processes. The concept that the structure of a biological molecule leads to function is a core principle of the biochemical field. Visualisation of biological molecules often involves vocal explanations or the use of two dimensional slides and video presentations. A deeper understanding of these molecules can however be obtained by the handling of objects. 3D printed biological molecules can be used as active learning tools to stimulate engagement in large group lectures. These models can be used to build upon initial core knowledge which can be delivered in either a flipped form or a more didactic manner. Within the teaching session the students are able to learn by handling, rotating and viewing the objects to gain an appreciation, for example, of an enzyme’s active site or the difference between the major and minor groove of DNA. Models and other artefacts can be handled in small groups within a lecture theatre and act as a focal point to generate conversation. Through the approach presented here core knowledge is first established and then supplemented with high level problem solving through a "Think-Pair-Share" cooperative learning strategy. The teaching delivery was adjusted based around experiential learning activities by moving the object from mental cognition and into the physical environment. This approach led to students being able to better visualise biological molecules and a positive engagement in the lecture. The use of objects in teaching allows the lecturer to create interactive sessions that both challenge and enable the student.

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Stan, Adina Dora, Codruta Birle, and Dana Slavoaca. "Biological molecules in clinical stroke trials." Romanian Journal of Neurology 12, no. 4 (December 31, 2013): 175–79. http://dx.doi.org/10.37897/rjn.2013.4.2.

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Stroke remains a leading cause of disability and mortality all over the world despite the efforts made towards improving treatment. Most of the clinical studies have not shown significant beneficial effects in the evaluation of various molecules for their neuroprotection and neuro-recovery promoting properties. The new concept of multimodal, pleiotropic drugs has opened new perspectives in this field. This review focuses on clinical stroke studies with biologically active molecules such as erythropoietin, granulocyte-colony stimulating factor and Cerebrolysin.

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Pushpanathan, Muthuirulan, Paramasamy Gunasekaran, and Jeyaprakash Rajendhran. "Antimicrobial Peptides: Versatile Biological Properties." International Journal of Peptides 2013 (June 26, 2013): 1–15. http://dx.doi.org/10.1155/2013/675391.

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Antimicrobial peptides are diverse group of biologically active molecules with multidimensional properties. In recent past, a wide variety of AMPs with diverse structures have been reported from different sources such as plants, animals, mammals, and microorganisms. The presence of unusual amino acids and structural motifs in AMPs confers unique structural properties to the peptide that attribute for their specific mode of action. The ability of these active AMPs to act as multifunctional effector molecules such as signalling molecule, immune modulators, mitogen, antitumor, and contraceptive agent makes it an interesting candidate to study every aspect of their structural and biological properties for prophylactic and therapeutic applications. In addition, easy cloning and recombinant expression of AMPs in heterologous plant host systems provided a pipeline for production of disease resistant transgenic plants. Besides these properties, AMPs were also used as drug delivery vectors to deliver cell impermeable drugs to cell interior. The present review focuses on the diversity and broad spectrum antimicrobial activity of AMPs along with its multidimensional properties that could be exploited for the application of these bioactive peptides as a potential and promising drug candidate in pharmaceutical industries.

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Cyphert, Jaime M., Carol S. Trempus, and Stavros Garantziotis. "Size Matters: Molecular Weight Specificity of Hyaluronan Effects in Cell Biology." International Journal of Cell Biology 2015 (2015): 1–8. http://dx.doi.org/10.1155/2015/563818.

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Hyaluronan signaling properties are unique among other biologically active molecules, that they are apparently not influenced by postsynthetic molecular modification, but by hyaluronan fragment size. This review summarizes the current knowledge about the generation of hyaluronan fragments of different size and size-dependent differences in hyaluronan signaling as well as their downstream biological effects.

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Fotopoulos, Ioannis, and Dimitra Hadjipavlou-Litina. "Hybrids of Coumarin Derivatives as Potent and Multifunctional Bioactive Agents: A Review." Medicinal Chemistry 16, no. 3 (April 17, 2020): 272–306. http://dx.doi.org/10.2174/1573406415666190416121448.

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Background: Coumarins exhibit a plethora of biological activities, e.g. antiinflammatory and anti-tumor. Molecular hybridization technique has been implemented in the design of novel coumarin hybrids with several bioactive groups in order to obtain molecules with better pharmacological activity and improved pharmacokinetic profile. Objective: Therefore, we tried to gather as many as possible biologically active coumarin hybrids referred in the literature till now, to delineate the structural characteristics in relation to the activities and to have a survey that might help the medicinal chemists to design new coumarin hybrids with drug-likeness and varied bioactivities. Results: The biological activities of the hybrids in most of the cases were found to be different from the biological activities presented by the parent coumarins. The results showed that the hybrid molecules are more potent compared to the standard drugs used in the evaluation experiments. Conclusion: Conjugation of coumarin with varied pharmacophore groups/druglike molecules responsible for different biological activities led to many novel hybrid molecules, with a multitarget behavior and improved pharmacokinetic properties.

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Zatloukalová, Martina. "3D Lipidic Matrix for Incorporation and Stabilization of Biologically Active Molecules." Chemické listy 116, no. 3 (March 15, 2022): 172–79. http://dx.doi.org/10.54779/chl20220172.

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In aqueous media, biologically active substances are usually unstable, poorly soluble compounds with low bioavailability. Incorporation of these compounds into the structure of lipid-based lyotropic liquid crystalline phase or nanoparticles can increase their solubility and subsequent bioavailability. The aim of this review is to clarify the principle of self-assembly of lipidic amphiphilic molecules in the aqueous environment, to present lipid bicontinuous cubic and hexagonal phases and their current biological application.

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Li, L., and P. K. Moore. "An overview of the biological significance of endogenous gases: new roles for old molecules." Biochemical Society Transactions 35, no. 5 (October 25, 2007): 1138–41. http://dx.doi.org/10.1042/bst0351138.

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Biologically active gases that occur naturally in the body include nitric oxide (NO), carbon monoxide (CO) and hydrogen sulfide (H2S). Each of these molecules is synthesized by enzymes which have been characterized biochemically and pharmacologically, and each acts, via well-established molecular targets, to effect physiological and/or pathophysiological functions within the body. Major biological roles that appear to be common to all three gases include the regulation of vascular homoeostasis and central nervous system function. It is becoming increasingly clear that both the synthesis and the biological activity of each gas are, to some extent, regulated by the presence of the others, and as such it is necessary to consider these molecules not in isolation but acting together to control cell function. Additional, more speculative candidates for gaseous cell signalling molecules include ammonia, acetaldehyde, sulfur dioxide and nitrous oxide. Whether such molecules also play a role in regulating body function remains to be determined.

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Оглобліна, М. В., І. В. Бушуєва, and В. В. Парченко. "Review of the research on the influence of different functional substituents of new 1,2,4-triazole derivatives on the compounds biological properties." Farmatsevtychnyi zhurnal, no. 5 (October 29, 2022): 74–80. http://dx.doi.org/10.32352/0367-3057.5.22.08.

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Today, 1,2,4-triazole derivatives are a promising class of organic compounds. This is caused, first of all, by the possibility of various chemical modifications of the 1,2,4-triazole fragment due to the addition of typical pharmacophores, which contributes to the expansion of the new molecules’ arsenal. A significant number of the 1,2,4-triazole derivatives show biological properties, that postively affects the further process of the most promising substances’ introduction. The aim of the work was to analyze the influence of various functional substituents of the new 1,2,4-triazole derivatives on the indicators of the mentioned compounds’ biological activity. Literature sources containing information on the influence of various functional substituents of the new 1,2,4-triazole derivatives on the indicators of these compounds’ biological activity became the research materials. Methods were used in the work: analytical, bibliosemantic information search, generalization. Triazoles and their heterocyclic analogues are compounds that contain a certain amount of Nitrogen atoms in their composition, showing the properties of typical pharmacophores. Their derivatives are easily synthesized and can be transformed into various biologically active molecules. Information on the 1,2,4-triazole derivatives’ chemical modeling, which allows for purposefully obtaining compounds with the necessary biological properties, taking into account the toxicity indicators of new molecules, has been analyzed and summarized. The authors have proved, that the gradual and predicted introduction of various substituents into the molecule of 1,2,4-triazole derivatives leads to the appearance of new types of biological activity, in some cases it gives an increase in already existing activity indicators. Chemical compounds’ modification due to the substituents’ changing around the 1,2,4-triazole fragment fundamentally changes the type of biological activity of new molecules. This approach was chosen by the majority of scientists as promising one for the new biologically active substances’ search among the 1,2,4-triazole derivatives. The priority, relevance and perspective of such researches have been proved by not only domestic scientists’ teams. Recently, foreign investigators from Turkey, India, Korea, China, Egypt, etc. have been actively searching for new biologically active substances among the 1,2,4-triazole derivatives. The analysis of modern literary sources on the study of the new 1,2,4-triazole derivatives’ biological activity allows us to establish certain features of the various functional substituents’ influence on the types of biological activity and convincingly proves the outlook of further synthetic tests in the compounds’ specified series.

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Kottalanka, Ravi K., Eswar Pagadala, Shiva K. Loke, S. Rex Jeya Rajkumar, Venkatesan Srinivasadesikan, and Balajee Ramchandran. "Biological Evolution of Titanium(IV) Complex [{(NNO)2Ti}3O3] Bearing Bidentate Heteroditopic Schiff Base Ligand: Synthesis, Structure and Biological Studies." Asian Journal of Chemistry 32, no. 2 (December 30, 2019): 441–50. http://dx.doi.org/10.14233/ajchem.2020.22464.

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Titanium(IV)-complex of chemical composition [{(NNO)2Ti}3O3] (2) bearing bidentate heteroditopic Schiff base [(C5H4OH)-N=CH-C4H3-NH] (L1) ligand in titanium coordination sphere was reported and its biological significance was evaluated. The in vitro cytotoxicity of L1 and 2 were evaluated by using MTT assay on cancer cell lines (MCF-7 & A549) and observed significant cytotoxicity. Further, the LDH and NO assay studies on both L1 and 2 on cancer cell lines revealed that the enhanced cytotoxicity compared to standard anticancer drug i.e. cisplatin. The DNA binding studies of tested compounds with Ct-DNA molecule by using UV-visible and fluorescence spectra and molecular docking studies revealed that moderate to good binding interactions with test molecules. Thus, the present work contributes and implies the biological significance of Ti-complex (2) and the correlation between the structure and the biological activities of such Ti-complexes supported by Schiff base systems opens up opportunities for further exploitation of similar biologically active titanium systems.

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Ziarani, Ghodsi M., Fatemeh Mohajer, Razieh Moradi, and Parisa Mofatehnia. "The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds." Current Organic Synthesis 16, no. 7 (December 26, 2019): 953–67. http://dx.doi.org/10.2174/1570179416666190925162215.

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Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

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Hansen, Poul Erik. "Structural Studies of β-Diketones and Their Implications on Biological Effects." Pharmaceuticals 14, no. 11 (November 20, 2021): 1189. http://dx.doi.org/10.3390/ph14111189.

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The paper briefly summarizes methods to determine the structure of β-diketones with emphasis on NMR methods. Density functional calculations are also briefly treated. Emphasis is on the tautomeric equilibria of β-diketones in relation to biological effects. Relevant physical parameters such as acidity and solubility are treated. A series of biologically active molecules are treated with respect to structure (tautomerism). Characteristic molecules or groups of molecules are usnic acids, tetramic and tetronic acids, o-hydroxydibenzoylmethanes, curcumines, lupulones, and hyperforines.

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Patel, Geetika, and Subhash Banerjee. "Review on Synthesis of Bio-active Coumarin-fused Heterocyclic Molecules." Current Organic Chemistry 24, no. 22 (December 18, 2020): 2566–87. http://dx.doi.org/10.2174/1385272824999200709125717.

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The literature survey reveals that the individual coumarin and heterocyclic molecules have biological and pharmaceutical activities. Moreover, integrated coumarinfused heterocyclic compounds have shown interesting biological and physiochemical properties and thus, designing and development of coumarin-fused heterocyclic molecules are of great interest in the field of synthetic organic chemistry. Several coumarin-fused heterocyclic molecules have been synthesized by using different strategies such as multistep method, one-pot multi-component protocol, coupling and condensation method. The wide applications of integrated coumarin-fused heterocyclic molecules stimulated interest among researchers to develop different methodologies for the synthesis of novel fused molecules. As a consequence, several research articles, papers and review articles have been published in the literature. In this review article, we have presented various methods for the synthesis of different class of coumarin-fused heterocyclic molecules and their applications in chemical, optical, pharmaceutical and other useful applications.

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Srivastava, Ambrish Kumar, and Neeraj Misra. "A comparative theoretical study on the biological activity, chemical reactivity, and coordination ability of dichloro-substituted (1,3-thiazol-2-yl)acetamides." Canadian Journal of Chemistry 92, no. 3 (March 2014): 234–39. http://dx.doi.org/10.1139/cjc-2013-0335.

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We present a theoretical study on three dichloro-substituted (1,3-thiazol-2-yl)acetamides using the first principle density functional approach. Natural bonding orbital analysis is used to discuss the coordination ability of molecules and various global reactivity descriptors are calculated to compare their chemical reactivity. Biological activities of all three molecules are also evaluated. We find that the present molecules show potential coordination ability and their chemical reactivity varies with the position of substitution. We also notice that all three molecules show remarkable biological activities and the (3,4)-dichloro-substituted molecule is relatively more active. The study suggests further investigations on these molecules for their pharmacological importance.

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Sandhya, P. V., K. V. Satheesh Kumar, and K. R. Haridas. "Synthesis, Molecular Docking and DFT Studies of Biologically Active N-((3-(4-Nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)aniline Derivatives." Asian Journal of Chemistry 34, no. 2 (2022): 297–304. http://dx.doi.org/10.14233/ajchem.2022.23500.

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Some biologically active pyrazole clubbed imino molecules have been designed and synthesized from 1-phenyl-3-nitro phenyl-1H- pyrazol-4-carboxaldehyde and substituted aromatic amines via acid catalyzed condensation reaction. All the synthesized molecules were characterized by IR, 1H NMR, 13C NMR and mass spectral techniques. The in vitro antibactericidal property of the synthesized compounds was screened and compared with the results of theoretical molecular docking. Optimization of molecular geometry, DNA binding interaction and FMO analysis were also investigated by computational studies using Gaussian 16 package at B3LYP/6-31G(d,p) level. All the synthesized compounds exhibited moderate to good biological activities both experimentally and theoretically.

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de Oliveira Costa, Bruna, and Octávio Luiz Franco. "Cryptic Host Defense Peptides: Multifaceted Activity and Prospects for Medicinal Chemistry." Current Topics in Medicinal Chemistry 20, no. 14 (June 11, 2020): 1274–90. http://dx.doi.org/10.2174/1568026620666200325112425.

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Host defense peptides (HDPs) comprise a heterogeneous group of evolutionarily conserved and biologically active small molecules that are produced by different organisms. HDPs are widely researched because they often have multiple biological activities, for example antimicrobial, immunomodulatory and anticancer activity. In this context, in this review we focus on cryptic HDPs, molecules derived specifically from proteolytic processing of endogenous precursor proteins. Here, we explore the biological activity of such molecules and we further discuss the development of optimized sequences based on these natural cryptic HDPs. In addition, we present clinical-phase studies of cryptic HDPs (natural or optimized), and point out the possible applicability of these molecules in medicinal chemistry.

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Belyakova, L. A., A. M. Varvarin, D. Yu Lyashenko, and O. V. Khora. "Designing Adsorption Centres for Biological Active Molecules on a Silica Surface." Adsorption Science & Technology 23, no. 9 (November 2005): 703–19. http://dx.doi.org/10.1260/026361705776316596.

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The chemical interaction between the surface of hydroxylated or aminated silicas and β-cyclodextrin, mono-tosyl-β-cyclodextrin and the bromine derivative of heptakis-[6- O-( p-tosyl-β-cyclodextrin)] has been investigated using IR spectroscopy, thermogravimetric analysis with programmed heating, pH titration, weight adsorption method, elemental analysis and quantitative chemical analysis of the surface compounds. The optimum conditions for chemical grafting of β-cyclodextrins onto the silica surface were established. The formation of supramolecular structures, viz. inclusion complexes between immobilized β-cyclodextrin and the hormone of pineal gland (melatonin), on the surface of highly dispersed silicas of 1:1 composition was demonstrated.

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Polat, M. Fatih. "Synthesis of Asebogenin and Balsacone A Precursor by a Novel Synthetic Strategy: Recent Opportunities for and Challenges of Total Synthesis of Balsacone A." Molecules 27, no. 11 (May 30, 2022): 3523. http://dx.doi.org/10.3390/molecules27113523.

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One of the main areas of interest of synthetic organic chemistry is the rapid construction of small molecules with proven diverse biological activities for the development of new strategies to cure human health. In particular, the development of novel synthetic strategies is the most important option for reaching the molecular scaffolds of active molecules of natural origin. Balsacone A and asebogenin are compounds that exhibit a wide variety of important biological activities. In this respect, it has become very important to develop new strategies for the construction of biologically active natural and synthetic balsacone analogues. In particular, balsacone derivatives with hydroxy-substituted dihydrochalcone skeletons can be isolated from plant sources or obtained by hemi-syntheses using bio-sourced precursors. An efficient synthetic strategy to synthetically obtain balsacone A is the aim of the present study that considers the limited natural availability of these molecules as well as other factors, such as cost and time. Starting with phloroglucinol, a nine-step synthesis of the precursor of balsacone A was achieved at a 10% overall yield. Furthermore, asebogenin, which has a dihydrochalcone structure and plays a key role in the synthesis of balsacone A, was synthesised with a good yield.

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Dumpis, Marina A., Dmitrii N. Nikolayev, Elena V. Litasova, Viktor V. Iljin, Mariya A. Brusina, and Levon B. Piotrovsky. "Biological activity of fullerenes - reality and prospects." Reviews on Clinical Pharmacology and Drug Therapy 16, no. 1 (March 15, 2018): 4–20. http://dx.doi.org/10.17816/rcf1614-20.

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The review deals with the properties of fullerenes and their derivatives and the possibility of their use in biology and medicine. Fullerenes can exert an antioxidant effect in biological systems, catching active forms of oxygen, and oxidative, giving the fullerene photosensitizing properties. The lipophilic fullerene molecules possessing membrane - tropic action interact with various biological structures and can change the functions of these structures, increasing the lipophilicity of the active molecule (amino acids, nucleic acids, proteins, etc.). Data on the biological effect of fullerenes in in vitro and in vivo experiments are given. Examples of targeted delivery of known therapeutic agents. (For citation: Dumpis MA, Nikolaev DN, Litasova EV, et al. Biological activity of fullerenes - reality and prospects. Reviews on Clinical Pharmacology and Drug Therapy. 2018;16(1):4-20. doi: 10.17816/RCF1614-20).

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Bisha, Ina, and Alessandra Magistrato. "The molecular mechanism of secondary sodium symporters elucidated through the lens of the computational microscope." RSC Advances 6, no. 12 (2016): 9522–40. http://dx.doi.org/10.1039/c5ra22131e.

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Transport of molecules across cellular membranes is a key biological process for normal cell function. In this review we describe current state-of-the-art knowledge on molecular mechanism of secondary active transporters obtained by molecular simulations studies.

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Skoreński, Marcin, and Marcin Sieńczyk. "The Fellowship of Privileged Scaffolds—One Structure to Inhibit Them All." Pharmaceuticals 14, no. 11 (November 16, 2021): 1164. http://dx.doi.org/10.3390/ph14111164.

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Over the past few years, the application of privileged structure has emerged as a powerful approach to the discovery of new biologically active molecules. Privileged structures are molecular scaffolds with binding properties to the range of different biological targets. Moreover, privileged structures typically exhibit good drug-like properties, thus assuring more drug-like properties of modified compound. Our main objective is to discuss the privileged structures used for the development of antiviral agents.

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Maestro, Aitor, Xabier del Corte, Adrián López-Francés, Edorta Martínez de Marigorta, Francisco Palacios, and Javier Vicario. "Asymmetric Synthesis of Tetrasubstituted α-Aminophosphonic Acid Derivatives." Molecules 26, no. 11 (May 27, 2021): 3202. http://dx.doi.org/10.3390/molecules26113202.

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Due to their structural similarity with natural α-amino acids, α-aminophosphonic acid derivatives are known biologically active molecules. In view of the relevance of tetrasubstituted carbons in nature and medicine and the strong dependence of the biological activity of chiral molecules into their absolute configuration, the synthesis of α-aminophosphonates bearing tetrasubstituted carbons in an asymmetric fashion has grown in interest in the past few decades. In the following lines, the existing literatures for the synthesis of optically active tetrasubstituted α-aminophosphonates are summarized, comprising diastereoselective and enantioselective approaches.

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Lee, Alpha A., Qingyi Yang, Asser Bassyouni, Christopher R. Butler, Xinjun Hou, Stephen Jenkinson, and David A. Price. "Ligand biological activity predicted by cleaning positive and negative chemical correlations." Proceedings of the National Academy of Sciences 116, no. 9 (February 11, 2019): 3373–78. http://dx.doi.org/10.1073/pnas.1810847116.

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Predicting ligand biological activity is a key challenge in drug discovery. Ligand-based statistical approaches are often hampered by noise due to undersampling: The number of molecules known to be active or inactive is vastly less than the number of possible chemical features that might determine binding. We derive a statistical framework inspired by random matrix theory and combine the framework with high-quality negative data to discover important chemical differences between active and inactive molecules by disentangling undersampling noise. Our model outperforms standard benchmarks when tested against a set of challenging retrospective tests. We prospectively apply our model to the human muscarinic acetylcholine receptor M1, finding four experimentally confirmed agonists that are chemically dissimilar to all known ligands. The hit rate of our model is significantly higher than the state of the art. Our model can be interpreted and visualized to offer chemical insights about the molecular motifs that are synergistic or antagonistic to M1 agonism, which we have prospectively experimentally verified.

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Kakou Yao, Rita, Jules Abodou Tenon, and Akoun Abou. "Bioactive molecules modelised by numerical simulation:molecules against Escherichia Coli." Acta Crystallographica Section A Foundations and Advances 70, a1 (August 5, 2014): C1008. http://dx.doi.org/10.1107/s2053273314089918.

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The work exposed in this paper joins in the research of medecine by means of the modelling by digital simulation (method in silico). This method allows to plan the biological activities of new molecules and to design others more active than existing molecules against a given infection . The generated and validated models are used here in the research for molecules potentially more active against Escherichia coli which causes diarrheic infections at the human beings. Here, we report works the synthesis of our works of structural determination, of forecast of biological activity and conception of molecules bioactive again Eschericha coli.

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Rydel-Ciszek, Katarzyna, Tomasz Pacześniak, Izabela Zaborniak, Paweł Błoniarz, Karolina Surmacz, Andrzej Sobkowiak, and Paweł Chmielarz. "Iron-Based Catalytically Active Complexes in Preparation of Functional Materials." Processes 8, no. 12 (December 20, 2020): 1683. http://dx.doi.org/10.3390/pr8121683.

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Iron complexes are particularly interesting as catalyst systems over the other transition metals (including noble metals) due to iron’s high natural abundance and mediation in important biological processes, therefore making them non-toxic, cost-effective, and biocompatible. Both homogeneous and heterogeneous catalysis mediated by iron as a transition metal have found applications in many industries, including oxidation, C-C bond formation, hydrocarboxylation and dehydration, hydrogenation and reduction reactions of low molecular weight molecules. These processes provided substrates for industrial-scale use, e.g., switchable materials, sustainable and scalable energy storage technologies, drugs for the treatment of cancer, and high molecular weight polymer materials with a predetermined structure through controlled radical polymerization techniques. This review provides a detailed statement of the utilization of homogeneous and heterogeneous iron-based catalysts for the synthesis of both low and high molecular weight molecules with versatile use, focusing on receiving functional materials with high potential for industrial application.

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Cetin, Adnan, and Havva Kurt. "Synthesis, Antibacterial Activity and Molecular Docking Studies of New Pyrazole Derivatives." Letters in Drug Design & Discovery 17, no. 6 (June 29, 2020): 745–56. http://dx.doi.org/10.2174/1570180816666190905155510.

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Background: The pyrazole structure is an important heterocyclic structure and plays critical roles in agriculture, industrial and medicine. Furthermore, compounds containing pyrazole are known to exhibit various biological properties such as antibacterial, antifungal, anticancer, antiinflammatory, antidepressant, antipyretic, antiviral, anti-tubercular and anti-HIV activities. Because of these properties, pyrazole molecules have become a very popular topic for organic chemists. Methods: A series newly substituted pyrazole molecules were synthesized and characterized. Their antimicrobial activities were investigated by disk diffusion method against some gram positive bacteria and gram negative bacteria. Results: The present results indicated that the some test compounds were active in a broad spectrum against important human pathogenic microorganisms. The substituted pyrazoles including carbazone (7a, b) and thiazolidine (8a, b) showed a wide variety of biological activities. The results showed that synthesized pyrazole, compounds 7b and 8b are highly active and more potent in both biological and molecular docking simulation studies. Conclusion: The synthesized pyrazole molecules showed moderate antibacterial activities against the tested microorganism compared to antibiotic drug. Some test compounds (7b and 8b) might be used as new antibacterial agents.

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Coelho, Simao, Jongho Baek, Matthew S. Graus, James M. Halstead, Philip R. Nicovich, Kristen Feher, Hetvi Gandhi, J. Justin Gooding, and Katharina Gaus. "Ultraprecise single-molecule localization microscopy enables in situ distance measurements in intact cells." Science Advances 6, no. 16 (April 2020): eaay8271. http://dx.doi.org/10.1126/sciadv.aay8271.

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Single-molecule localization microscopy (SMLM) has the potential to quantify the diversity in spatial arrangements of molecules in intact cells. However, this requires that the single-molecule emitters are localized with ultrahigh precision irrespective of the sample format and the length of the data acquisition. We advance SMLM to enable direct distance measurements between molecules in intact cells on the scale between 1 and 20 nm. Our actively stabilized microscope combines three-dimensional real-time drift corrections and achieves a stabilization of <1 nm and localization precision of ~1 nm. To demonstrate the biological applicability of the new microscope, we show a 4- to 7-nm difference in spatial separations between signaling T cell receptors and phosphatases (CD45) in active and resting T cells. In summary, by overcoming the major bottlenecks in SMLM imaging, it is possible to generate molecular images with nanometer accuracy and conduct distance measurements on the biological relevant length scales.

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Montuori, Nunzia, Valeria Visconte, Guido Rossi, and Pia Ragno. "Soluble and cleaved forms of the urokinase-receptor: degradation products or active molecules?" Thrombosis and Haemostasis 93, no. 02 (2005): 192–98. http://dx.doi.org/10.1160/th04-09-0580.

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SummaryThe urokinase-mediated plasminogen activation (PA) system is involved in many physiological and pathological events that include cell migration and tissue remodelling, such as embryogenesis, ovulation, inflammation, wound healing, angiogenesis, and tumor invasion and metastasis. The urokinase receptor (uPAR) is a key molecule of this system and can bind extracellular and cell membrane molecules such as urokinase (uPA), vitronectin (VN), integrins and chemotaxis receptors. These multiple interactions can be modulated by the shedding or the cleavage of the cell membrane receptor. Indeed, cleaved forms of uPAR, lacking the N-terminal D1 domain, have been detected on the surface of cells and in tissues, while soluble forms have been found in biological fluids. Cleaved and soluble forms could represent the intermediary products of the uPAR metabolism or active molecules with precise and distinct functional roles. Here, we review the data concerning the in vitro and in vivo identification of these uPAR forms, their origin and functions, and the role that uPAR shedding and cleavage could play in biological processes.

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Katsuyama, Isamu. "Synthesis of Trifluoromethyl-Containing Pyridines and Their Applications to Biological Active Molecules." Journal of Synthetic Organic Chemistry, Japan 67, no. 10 (2009): 992–1000. http://dx.doi.org/10.5059/yukigoseikyokaishi.67.992.

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Flood, P. M., C. Waltenbaugh, T. Tada, B. Chue, and D. B. Murphy. "Serologic heterogeneity in I-J determinants associated with functionally distinct T cell regulatory factors." Journal of Immunology 137, no. 7 (October 1, 1986): 2237–44. http://dx.doi.org/10.4049/jimmunol.137.7.2237.

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Abstract Information transfer among regulatory T cell subsets is mediated by biologically active T cell factors. Many of these factors are comprised of two molecules: one that binds antigen, and another that is I-J+ and determines the self recognition capability of the factor (I-J molecule). In the in vitro response to sheep red blood cells, we used three functionally distinct I-J+ factors to study the relationship between polymorphic I-J determinants and the biological activity of these factors. Our study shows that several monoclonal I-J antibodies react with I-J molecules associated with T suppressor-inducer factor (TsiF) and T suppressor-effector factor (TseF), but not with T contrasuppressor inducer factor (TcsiF). In contrast, a different set of monoclonal I-J reagents reacts with TcsiF but not TsiF or TseF. Finally, some monoclonal I-J antibodies distinguish between I-J molecules associated with TsiF and TseF. Thus anti-I-J reagents differentially react with I-J determinants on regulatory factors, and this differential pattern of reactivity correlates with the functional activity of the factors. The possible relationship between I-J heterogeneity and the biological function of I-J molecules in regulation is discussed.

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Kalasariya, Haresh S., Virendra Kumar Yadav, Krishna Kumar Yadav, Vineet Tirth, Ali Algahtani, Saiful Islam, Neha Gupta, and Byong-Hun Jeon. "Seaweed-Based Molecules and Their Potential Biological Activities: An Eco-Sustainable Cosmetics." Molecules 26, no. 17 (September 1, 2021): 5313. http://dx.doi.org/10.3390/molecules26175313.

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Amongst the countless marine organisms, seaweeds are considered as one of the richest sources of biologically active ingredients having powerful biological activities. Seaweeds or marine macroalgae are macroscopic multicellular eukaryotic photosynthetic organisms and have the potential to produce a large number of valuable compounds, such as proteins, carbohydrates, fatty acids, amino acids, phenolic compounds, pigments, etc. Since it is a prominent source of bioactive constituents, it finds diversified industrial applications viz food and dairy, pharmaceuticals, medicinal, cosmeceutical, nutraceutical, etc. Moreover, seaweed-based cosmetic products are risen up in their demands by the consumers, as they see them as a promising alternative to synthetic cosmetics. Normally it contains purified biologically active compounds or extracts with several compounds. Several seaweed ingredients that are useful in cosmeceuticals are known to be effective alternatives with significant benefits. Many seaweeds’ species demonstrated skin beneficial activities, such as antioxidant, anti-melanogenesis, antiaging, photoprotection, anti-wrinkle, moisturizer, antioxidant, anti-inflammatory, anticancer and antioxidant properties, as well as certain antimicrobial activities, such as antibacterial, antifungal and antiviral activities. This review presents applications of bioactive molecules derived from marine algae as a potential substitute for its current applications in the cosmetic industry. The biological activities of carbohydrates, proteins, phenolic compounds and pigments are discussed as safe sources of ingredients for the consumer and cosmetic industry.

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Hegedüs, Imre, Kitti Andreidesz, József L. Szentpéteri, Zoltán Kaleta, László Szabó, Krisztián Szigeti, Balázs Gulyás, Parasuraman Padmanabhan, Ferenc Budan, and Domokos Máthé. "The Utilization of Physiologically Active Molecular Components of Grape Seeds and Grape Marc." International Journal of Molecular Sciences 23, no. 19 (September 22, 2022): 11165. http://dx.doi.org/10.3390/ijms231911165.

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Nutritional interventions may highly contribute to the maintenance or restoration of human health. Grapes (Vitis vinifera) are one of the oldest known beneficial nutritional components of the human diet. Their high polyphenol content has been proven to enhance human health beyond doubt in statistics-based public health studies, especially in the prevention of cardiovascular disease and cancer. The current review concentrates on presenting and classifying polyphenol bioactive molecules (resveratrol, quercetin, catechin/epicatechin, etc.) available in high quantities in Vitis vinifera grapes or their byproducts. The molecular pathways and cellular signaling cascades involved in the effects of these polyphenol molecules are also presented in this review, which summarizes currently available in vitro and in vivo experimental literature data on their biological activities mostly in easily accessible tabular form. New molecules for different therapeutic purposes can also be synthesized based on existing polyphenol compound classes available in high quantities in grape, wine, and grape marc. Therefore an overview of these molecular structures is provided. Novel possibilities as dendrimer nanobioconjugates are reviewed, too. Currently available in vitro and in vivo experimental literature data on polyphenol biological activities are presented in easily accessible tabular form. The scope of the review details the antidiabetic, anticarcinogenic, antiviral, vasoprotective, and neuroprotective roles of grape-origin flavonoids. The novelty of the study lies in the description of the processing of agricultural by-products (grape seeds and skins) of industrial relevance, and the detailed description of the molecular mechanisms of action. In addition, the review of the clinical therapeutic applications of polyphenols is unique as no summary study has yet been done.

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Luo, Huiqing, Na Li, Liyan Liu, Huaqiao Wang, and Feng He. "Synthesis of New AIEE-Active Chalcones for Imaging of Mitochondria in Living Cells and Zebrafish In Vivo." International Journal of Molecular Sciences 22, no. 16 (August 19, 2021): 8949. http://dx.doi.org/10.3390/ijms22168949.

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Fluorophores with aggregation-induced emission enhancement (AIEE) properties have attracted increasing interest in recent years. On the basis of our previous research, we successfully designed and synthesized eleven chalcones. Through an optical performance experiment, we confirmed that compounds 1–6 had obvious AIEE properties. As these AIEE molecules had excellent fluorescence properties and a large Stokes shift, we studied their application in living cell imaging, and the results showed that these compounds had low cytotoxicity and good biocompatibility at the experimental concentrations. More importantly, they could specifically label mitochondria. Subsequently, we selected zebrafish as experimental animals to explore the possibilities of these compounds in animal imaging. The fluorescence imaging of zebrafish showed that these AIEE molecules can enter the embryo and can be targeted to aggregate in the digestive tract, which provides a strong foundation for their practical application in the field of biological imaging. Compared with traditional fluorophores, these AIEE molecules have the advantages of possessing a small molecular weight and high flexibility. Therefore, they have excellent application prospects in the field of biological imaging. In addition, the findings of this study have very positive practical significance for the discovery of more AIEE molecules.

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Morozkina, Svetlana N., Thi Hong Nhung Vu, Yuliya E. Generalova, Petr P. Snetkov, and Mayya V. Uspenskaya. "Mangiferin as New Potential Anti-Cancer Agent and Mangiferin-Integrated Polymer Systems—A Novel Research Direction." Biomolecules 11, no. 1 (January 9, 2021): 79. http://dx.doi.org/10.3390/biom11010079.

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For a long time, the pharmaceutical industry focused on natural biologically active molecules due to their unique properties, availability and significantly less side-effects. Mangiferin is a naturally occurring C-glucosylxantone that has substantial potential for the treatment of various diseases thanks to its numerous biological activities. Many research studies have proven that mangiferin possesses antioxidant, anti-infection, anti-cancer, anti-diabetic, cardiovascular, neuroprotective properties and it also increases immunity. It is especially important that it has no toxicity. However, mangiferin is not being currently applied to clinical use because its oral bioavailability as well as its absorption in the body are too low. To improve the solubility, enhance the biological action and bioavailability, mangiferin integrated polymer systems have been developed. In this paper, we review molecular mechanisms of anti-cancer action as well as a number of designed polymer-mangiferin systems. Taking together, mangiferin is a very promising anti-cancer molecule with excellent properties and the absence of toxicity.

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Morozkina, Svetlana N., Thi Hong Nhung Vu, Yuliya E. Generalova, Petr P. Snetkov, and Mayya V. Uspenskaya. "Mangiferin as New Potential Anti-Cancer Agent and Mangiferin-Integrated Polymer Systems—A Novel Research Direction." Biomolecules 11, no. 1 (January 9, 2021): 79. http://dx.doi.org/10.3390/biom11010079.

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For a long time, the pharmaceutical industry focused on natural biologically active molecules due to their unique properties, availability and significantly less side-effects. Mangiferin is a naturally occurring C-glucosylxantone that has substantial potential for the treatment of various diseases thanks to its numerous biological activities. Many research studies have proven that mangiferin possesses antioxidant, anti-infection, anti-cancer, anti-diabetic, cardiovascular, neuroprotective properties and it also increases immunity. It is especially important that it has no toxicity. However, mangiferin is not being currently applied to clinical use because its oral bioavailability as well as its absorption in the body are too low. To improve the solubility, enhance the biological action and bioavailability, mangiferin integrated polymer systems have been developed. In this paper, we review molecular mechanisms of anti-cancer action as well as a number of designed polymer-mangiferin systems. Taking together, mangiferin is a very promising anti-cancer molecule with excellent properties and the absence of toxicity.

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Dunkel, Petra. "Photoremovable Protecting Groups." Encyclopedia 2, no. 3 (July 1, 2022): 1225–36. http://dx.doi.org/10.3390/encyclopedia2030082.

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Photoremovable protecting groups (PPGs) (also often called photocages in the literature) are used for temporary inactivation of biologically active substrates. By photoirradiation the PPG could be cleaved off and the biological activity could be restored on-demand, with a high spatiotemporal precision. The on-site liberation of the biologically active substrate could be exploited for studying dynamic biological processes or for designing targeted pharmacological interventions in vitro or in vivo. Several chemical scaffolds have been described and tested as PPGs, operating at different wavelengths. The scope of potential substrates is very broad, spanning from small molecules to proteins. In a wider context, PPGs could be used for the design of various light-responsive materials as well, for diverse applications.

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Berlaga, Alex, and Anatoly B. Kolomeisky. "Theoretical study of active secondary transport: Unexpected differences in molecular mechanisms for antiporters and symporters." Journal of Chemical Physics 156, no. 8 (February 28, 2022): 085102. http://dx.doi.org/10.1063/5.0082589.

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Successful functioning of biological cells relies on efficient translocation of different materials across cellular membranes. An important part of this transportation system is membrane channels that are known as antiporters and symporters. They exploit the energy stored as a trans-membrane gradient of one type of molecules to transport the other types of molecules against their gradients. For symporters, the directions of both fluxes for driving and driven species coincide, while for antiporters, the fluxes move in opposite directions. There are surprising experimental observations that despite differing only by the direction of transport fluxes, the molecular mechanisms of translocation adopted by antiporters and symporters seem to be drastically different. We present chemical-kinetic models to quantitatively investigate this phenomenon. Our theoretical approach allows us to explain why antiporters mostly utilize a single-site transportation when only one molecule of any type might be associated with the channel. At the same time, the transport in symporters requires two molecules of different types to be simultaneously associated with the channel. In addition, we investigate the kinetic constraints and efficiency of symporters and compare them with the same properties of antiporters. Our theoretical analysis clarifies some important physical–chemical features of cellular trans-membrane transport.

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Asif, Mohammad. "Chemical Characteristics, Synthetic Methods, and Biological Potential of Quinazoline and Quinazolinone Derivatives." International Journal of Medicinal Chemistry 2014 (November 13, 2014): 1–27. http://dx.doi.org/10.1155/2014/395637.

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The heterocyclic fused rings quinazoline and quinazolinone have drawn a huge consideration owing to their expanded applications in the field of pharmaceutical chemistry. Quinazoline and quinazolinone are reported for their diversified biological activities and compounds with different substitutions bring together to knowledge of a target with understanding of the molecule types that might interact with the target receptors. Quinazolines and quinazolinones are considered as an important chemical for the synthesis of various physiological significance and pharmacological utilized molecules. Quinazolines and quinazolinone are a large class of biologically active compounds that exhibited broad spectrum of biological activities such as anti-HIV, anticancer, antifungal, antibacterial, antimutagenic, anticoccidial, anticonvulsant, anti-inflammatory, antidepressant, antimalarial, antioxidant, antileukemic, and antileishmanial activities and other activities. Being considered as advantaged scaffold, the alteration is made with different substituent.

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Nurkenov, O. A., S. D. Fazylov, G. K. Mukusheva, Ye V. Minayeva, I. V. Kulakov, Zh S. Nurmaganbetov, A. S. Kishkentaeva, and A. R. Zhasymbekova. "HYBRID MOLECULES BASED ON ALKALOIDS." Chemical Journal of Kazakhstan 3 (September 30, 2021): 67–82. http://dx.doi.org/10.51580/2021-1/2710-1185.40.

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This review has been summarized the data on the synthesis of new hybrid derivatives based on alkaloid molecules. At the same time, there have been analyzed methods for obtaining hybrid structures containing fragments of natural compounds molecules in combination with other biologically active plant metabolites, as leading compounds for the development of new pharmacologically valuable agents, with the aim of creating new original drugs. The combination of pharmacophoric residues in one molecule, namely various aromatic and heterocyclic substituents in the nucleoside position of natural alkaloids, opens up new possibilities for both the subsequent chemical modification of the polyfunctional derivatives obtained and their new diverse biological activity. Effective methods of synthesis have been developed on the basis of directed transformations of these compounds (or their precursors). A wide range of pharmaco-logical properties of combined compounds of these series with a combination of low toxicity is promising. Considering that the preparation of combined derivatives based on alkaloid molecules has been insufficiently studied, the targeted synthesis of new com-pounds is of interest both in terms of new medicinespreparation and the development of new methods of organic synthesis, as well as the molecules stereochemistry determination of a new series of compounds.

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Pagel, Mareen, and Annette G. Beck-Sickinger. "Multifunctional biomaterial coatings: synthetic challenges and biological activity." Biological Chemistry 398, no. 1 (January 1, 2017): 3–22. http://dx.doi.org/10.1515/hsz-2016-0204.

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Abstract A controlled interaction of materials with their surrounding biological environment is of great interest in many fields. Multifunctional coatings aim to provide simultaneous modulation of several biological signals. They can consist of various combinations of bioactive, and bioinert components as well as of reporter molecules to improve cell-material contacts, prevent infections or to analyze biochemical events on the surface. However, specific immobilization and particular assembly of various active molecules are challenging. Herein, an overview of multifunctional coatings for biomaterials is given, focusing on synthetic strategies and the biological benefits by displaying several motifs.

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Hansma, H. G., A. L. Weisenhorn, A. B. Edmundson, H. E. Gaub, and P. K. Hansma. "Atomic force microscopy: seeing molecules of lipid and immunoglobulin." Clinical Chemistry 37, no. 9 (September 1, 1991): 1497–501. http://dx.doi.org/10.1093/clinchem/37.9.1497.

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Abstract The atomic force microscope (AFM) can image individual molecules by raster-scanning a sharp tip over a surface. In this paper we present molecular-resolution images of immunoglobulin M (IgM) and of ultraviolet light-polymerized films of the lipid dimethyl-bis(pentacosadiynoyloxyethyl) ammonium bromide ("BRONCO"). The polar head groups of individual lipid molecules can be resolved on the surface of this and other lipid films. These lipid films also provide a good substrate for AFM imaging of DNA and of other molecules such as antibodies. Because the AFM scans surfaces, it is most often successful at imaging either molecules that can form an array on a surface or molecules that are quite firmly attached to a surface. The ability of the AFM to operate under water, buffers, and other liquids makes it possible to study biological molecules under conditions in which they are physiologically active. Imaging of the actual molecular process of fibrin polymerization shows the potential of the AFM for studying biological processes. In the six years since its invention, the AFM has excited much interest and has imaged molecules in a wide range of systems.

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Bian, Yuemin, and Xiang-Qun Xie. "Artificial Intelligent Deep Learning Molecular Generative Modeling of Scaffold-Focused and Cannabinoid CB2 Target-Specific Small-Molecule Sublibraries." Cells 11, no. 5 (March 7, 2022): 915. http://dx.doi.org/10.3390/cells11050915.

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Design and generation of high-quality target- and scaffold-specific small molecules is an important strategy for the discovery of unique and potent bioactive drug molecules. To achieve this goal, authors have developed the deep-learning molecule generation model (DeepMGM) and applied it for the de novo molecular generation of scaffold-focused small-molecule libraries. In this study, a recurrent neural network (RNN) using long short-term memory (LSTM) units was trained with drug-like molecules to result in a general model (g-DeepMGM). Sampling practices on indole and purine scaffolds illustrate the feasibility of creating scaffold-focused chemical libraries based on machine intelligence. Subsequently, a target-specific model (t-DeepMGM) for cannabinoid receptor 2 (CB2) was constructed following the transfer learning process of known CB2 ligands. Sampling outcomes can present similar properties to the reported active molecules. Finally, a discriminator was trained and attached to the DeepMGM to result in an in silico molecular design-test circle. Medicinal chemistry synthesis and biological validation was performed to further investigate the generation outcome, showing that XIE9137 was identified as a potential allosteric modulator of CB2. This study demonstrates how recent progress in deep learning intelligence can benefit drug discovery, especially in de novo molecular design and chemical library generation.

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Mikhailov, Alexander S., and Raymond Kapral. "Hydrodynamic collective effects of active protein machines in solution and lipid bilayers." Proceedings of the National Academy of Sciences 112, no. 28 (June 29, 2015): E3639—E3644. http://dx.doi.org/10.1073/pnas.1506825112.

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The cytoplasm and biomembranes in biological cells contain large numbers of proteins that cyclically change their shapes. They are molecular machines that can function as molecular motors or carry out various other tasks in the cell. Many enzymes also undergo conformational changes within their turnover cycles. We analyze the advection effects that nonthermal fluctuating hydrodynamic flows induced by active proteins have on other passive molecules in solution or membranes. We show that the diffusion constants of passive particles are enhanced substantially. Furthermore, when gradients of active proteins are present, a chemotaxis-like drift of passive particles takes place. In lipid bilayers, the effects are strongly nonlocal, so that active inclusions in the entire membrane contribute to local diffusion enhancement and the drift. All active proteins in a biological cell or in a membrane contribute to such effects and all passive particles, and the proteins themselves, will be subject to them.

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Caporali, Sabrina, Alessandro De Stefano, Cinzia Calabrese, Alfredo Giovannelli, Massimo Pieri, Isabella Savini, Manfredi Tesauro, Sergio Bernardini, Marilena Minieri, and Alessandro Terrinoni. "Anti-Inflammatory and Active Biological Properties of the Plant-Derived Bioactive Compounds Luteolin and Luteolin 7-Glucoside." Nutrients 14, no. 6 (March 9, 2022): 1155. http://dx.doi.org/10.3390/nu14061155.

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Flavonoids are interesting molecules synthetized by plants. They can be found abundantly in seeds and fruits, determining the color, flavor, and other organoleptic characteristics, as well as contributing to important nutritional aspects. Beyond these characteristics, due to their biochemical properties and characteristics, they can be considered bioactive compounds. Several interesting studies have demonstrated their biological activity in different cellular and physiological processes in high-order organisms including humans. The flavonoid molecular structure confers the capability of reacting with and neutralizing reactive oxygen species (ROS), behaving as scavengers in all processes generating this class of molecules, such as UV irradiation, a process widely present in plant physiology. Importantly, the recent scientific literature has demonstrated that flavonoids, in human physiology, are active compounds acting not only as scavengers but also with the important role of counteracting the inflammation process. Among the wide variety of flavonoid molecules, significant results have been shown by investigating the role of the flavones luteolin and luteolin-7-O-glucoside (LUT-7G). For these compounds, experimental results demonstrated an interesting anti-inflammatory action, both in vitro and in vivo, in the interaction with JAK/STAT3, NF-κB, and other pathways described in this review. We also describe the effects in metabolic pathways connected with inflammation, such as cellular glycolysis, diabetes, lipid peroxidation, and effects in cancer cells. Moreover, the inhibition of inflammatory pathway in endothelial tissue, as well as the NLRP3 inflammasome assembly, demonstrates a key role in the progression of such phenomena. Since these micronutrient molecules can be obtained from food, their biochemical properties open new perspectives with respect to the long-term health status of healthy individuals, as well as their use as a coadjutant treatment in specific diseases.

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Vanguru, Mahathy, Ramchander Merugu, Swetha Garimella, and Laxminarayana E. "A REVIEW ON THE SYNTHETIC METHODOLOGIES OF CHROMONES." Asian Journal of Pharmaceutical and Clinical Research 11, no. 12 (December 7, 2018): 9. http://dx.doi.org/10.22159/ajpcr.2018.v11i12.27960.

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Chromones group of compounds and their derivatives form the essential component of pharmacophores in many biologically active molecules. They exhibit a wide range of biological activities such as antibiotic, antitumor, antiviral, antioxidant, antipsychotic, and antihypoxic activities. These applications have stimulated a continuous search for the synthesis of new compounds in this field and are being extensively investigated. The various methodologies so far reported for the synthesis of these compounds with the compounds biological applications are discussed in this communication

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Hatchell, Tashi, Kasci Hutchenson, Gibin George, Zhiping Luo, and Shubo Han. "Morphological and Compositional Characterization of Electrochemically Active Perovskite Oxides for Sensing Biological Molecules." Microscopy and Microanalysis 26, S2 (July 30, 2020): 2664–65. http://dx.doi.org/10.1017/s1431927620022369.

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Journal articles on the topic 'Biological Active Molecules'

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