Bibliographies thématiques / Synthesis Novel Bioactive Steroids

Littérature scientifique sur le sujet « Synthesis Novel Bioactive Steroids »

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Publié le 6 septembre 2023

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Articles de revues sur le sujet "Synthesis Novel Bioactive Steroids"

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Silva, Gabriela A., Olga P. Coutinho, Paul Ducheyne, I. M. Shapiro et Rui L. Reis. « Starch-Based Microparticles as a Novel Strategy for Tissue Engineering Applications ». Key Engineering Materials 309-311 (mai 2006) : 907–10. http://dx.doi.org/10.4028/www.scientific.net/kem.309-311.907.

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Current tissue engineering strategies involve the use of scaffold materials with properties specific for the target tissue. When the tissue being treated is bone, properties such as bone bonding behaviour and excellent biological performance are very desirable. Many strategies involve the creation in vitro of a suitable hybrid construct (i.e., comprising a scaffold material and cells). These scaffolds are then inserted into the defect site, thus achieving faster integration and hence, repair. Herein, we describe the synthesis and characterization of starch-based microparticles for bone tissue engineering. This study describes the properties of two types of starch-based microparticles: their bioactivity in vitro (when processed with Bioactive Glass 45S5), the good biological performance and also the ability to be used as controlled release vehicles of bioactive molecules, such as steroids and growth factors.
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Berger, Andreas, Georg Petschenka, Thomas Degenkolb, Michael Geisthardt et Andreas Vilcinskas. « Insect Collections as an Untapped Source of Bioactive Compounds—Fireflies (Coleoptera : Lampyridae) and Cardiotonic Steroids as a Proof of Concept ». Insects 12, no 8 (31 juillet 2021) : 689. http://dx.doi.org/10.3390/insects12080689.

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Natural history collections provide an invaluable basis for systematics, ecology, and conservation. Besides being an important source of DNA, museum specimens may also contain a plethora of natural products. Especially, dried insect collections represent a global repository with billions of inventoried vouchers. Due to their vast diversity, insects possess a great variety of defensive compounds, which they either produce autogenously or derive from the environment. Here, we present a case study on fireflies (Coleoptera: Lampyridae), which produce bufadienolides as a defense against predators. These toxins belong to the cardiotonic steroids, which are used for the treatment of cardiac diseases and specifically inhibit the animal enzyme Na+/K+-ATPase. Bufadienolides have been reported from only seven out of approximately 2000 described firefly species. Using a non-destructive approach, we screened 72 dry coleopteran specimens for bufadienolides using HPLC-DAD and HPLC-MS. We found bufadienolides including five novel compounds in 21 species of the subfamily Lampyrinae. The absence of bufadienolides in the phylogenetically related net-winged beetles (Lycidae) and the lampyrid subfamilies Luciolinae and Lamprohizinae indicates a phylogenetic pattern of bufadienolide synthesis. Our results emphasize the value of natural history collections as an archive of chemical information for ecological and evolutionary basic research and as an untapped source for novel bioactive compounds.
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Larayetan, Rotimi, Zacchaeus S. Ololade, Oluranti O. Ogunmola et Ayodele Ladokun. « Phytochemical Constituents, Antioxidant, Cytotoxicity, Antimicrobial, Antitrypanosomal, and Antimalarial Potentials of the Crude Extracts of Callistemon citrinus ». Evidence-Based Complementary and Alternative Medicine 2019 (28 août 2019) : 1–14. http://dx.doi.org/10.1155/2019/5410923.

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Plants are reservoir for potentially useful bioactive compounds, and owing to the rising occurrences of drug resistance to malaria parasites, there is a need to discover and develop new phytochemicals in plant that can be used as antimalarial agents. In this study, we gave a detailed description of the phytochemicals present in both ethyl acetate and methanolic extracts of Callistemon citrinus (C. citrinus) using Gas Chromatography-Mass Spectrometry (GC-MS) analysis; both extracts were also evaluated for their in vitro antimalarial, antitrypanosomal, and cytotoxicity activities against Trypanosoma brucei brucei (T. b brucei) parasites, Plasmodium falciparum (P. falciparum) malaria parasites 3D7 strain, and human cervix adenocarcinoma cells (HeLa cells); in addition, the antimicrobial and antioxidant efficacies were determined using standard methods. Both extracts were characterized by a high amount of fatty acids (52.88 and 62.48%). The ethyl acetate extract exhibited a greater activity with minimum inhibitory concentration (MIC) values ranging from 0.025 to 0.10 mg/mL while the methanol extract ranged from 0.025 to 0.15 mg/mL. Both extracts were bactericidal to Escherichia coli ATCC 35150 (E. coli) and Pseudomonas aeruginosa ACC (P. aeruginosa). Qualitative and quantitative phytochemical screenings conducted for both extracts revealed the presence of alkaloids, glycosides, saponins, steroids, and triterpenoids, fat and oils, flavonoids, phenols, and tannins in varying amounts. Both crude extracts exhibited antitrypanosomal potentials with an IC50 of 6.6/9.7 μg/mL and antiplasmodial activities with an IC50 of 8.4/13.0 μg/mL. Conclusion from this study indicates that apart from the folkloric uses of this plant in traditional settings, the extracts possess a broad spectrum of antimicrobial, antitrypanosomal, and antimalarial activities and some pharmaceutically essential bioactive components with remarkable antioxidant capacities that may be used in the synthesis of novel drugs for the management of different varieties of ailments.
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Singh, Meenakshi, V. Ravichandiran, Yogesh P. Bharitkar et Abhijit Hazra. « Natural Products Containing Olefinic Bond : Important Substrates for Semi-synthetic Modification Towards Value Addition ». Current Organic Chemistry 24, no 7 (3 juin 2020) : 709–45. http://dx.doi.org/10.2174/1385272824666200312125734.

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: Semi-synthesis, the way of preparing novel bioactive molecules via modification of compounds isolated from natural sources is very much useful nowadays in the drug discovery process. The modification is based on the reaction of functional group(s) present in a natural compound. Among the examples of functional group transformation, double bond modification is also common in the literature. Several reactions like hydrogenation, cyclopropanation, epoxidation, addition reaction (halogenations, hydroxylation), Michael addition, Heck reaction, cycloaddition, dipolar cycloaddition, etc. are employed for this purpose. In this review, we have tried to gather the reactions performed with several double bond containing classes of natural products like diterpenes, xanthones, sesquiterpene exomethylene lactones, diaryl heptanoids, steroidal lactones, triterpenoids, limonoids, and alkamides. Where available, the effects of transformations on the biological activities of the molecules are also mentioned.
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Srivastava, Shubhi, et Paul A. K. « Associated microflora of medicinal ferns : biotechnological potentials and possible applications ». International Journal of Bioassays 5, no 03 (29 février 2016) : 4927. http://dx.doi.org/10.21746/ijbio.2016.03.0017.

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Plant associated microorganisms that colonize the upper and internal tissues of roots, stems, leaves and flowers of healthy plants without causing any visible harmful or negative effect on their host. Diversity of microbes have been extensively studied in a wide variety of vascular plants and shown to promote plant establishment, growth and development and impart resistance against pathogenic infections. Ferns and their associated microbes have also attracted the attention of the scientific communities as sources of novel bioactive secondary metabolites. The ferns and fern alleles, which are well adapted to diverse environmental conditions, produce various secondary metabolites such as flavonoids, steroids, alkaloids, phenols, triterpenoid compounds, variety of amino acids and fatty acids along with some unique metabolites as adaptive features and are traditionally used for human health and medicine. In this review attention has been focused to prepare a comprehensive account of ethnomedicinal properties of some common ferns and fern alleles. Association of bacteria and fungi in the rhizosphere, phyllosphere and endosphere of these medicinally important ferns and their interaction with the host plant has been emphasized keeping in view their possible biotechnological potentials and applications. The processes of host-microbe interaction leading to establishment and colonization of endophytes are less-well characterized in comparison to rhizospheric and phyllospheric microflora. However, the endophytes are possessing same characteristics as rhizospheric and phyllospheric to stimulate the in vivo synthesis as well as in vitro production of secondary metabolites with a wide range of biological activities such as plant growth promotion by production of phytohormones, siderophores, fixation of nitrogen, and phosphate solubilization. Synthesis of pharmaceutically important products such as anticancer compounds, antioxidants, antimicrobials, antiviral substances and hydrolytic enzymes could be some of the promising areas of research and commercial exploitation.
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Seferovic, Maxim D., Christine A. Beamish, Rockann E. Mosser, Shannon E. Townsend, Kirk Pappan, Vincent Poitout, Kjersti M. Aagaard et Maureen Gannon. « Increases in bioactive lipids accompany early metabolic changes associated with β-cell expansion in response to short-term high-fat diet ». American Journal of Physiology-Endocrinology and Metabolism 315, no 6 (1 décembre 2018) : E1251—E1263. http://dx.doi.org/10.1152/ajpendo.00001.2018.

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Pancreatic β-cell expansion is a highly regulated metabolic adaptation to increased somatic demands, including obesity and pregnancy; adult β cells otherwise rarely proliferate. We previously showed that high-fat diet (HFD) feeding induces mouse β-cell proliferation in less than 1 wk in the absence of insulin resistance. Here we metabolically profiled tissues from a short-term HFD β-cell expansion mouse model to identify pathways and metabolite changes associated with β-cell proliferation. Mice fed HFD vs. chow diet (CD) showed a 14.3% increase in body weight after 7 days; β-cell proliferation increased 1.75-fold without insulin resistance. Plasma from 1-wk HFD-fed mice induced β-cell proliferation ex vivo. The plasma, as well as liver, skeletal muscle, and bone, were assessed by LC and GC mass-spectrometry for global metabolite changes. Of the 1,283 metabolites detected, 159 showed significant changes [false discovery rate (FDR) < 0.1]. The majority of changes were in liver and muscle. Pathway enrichment analysis revealed key metabolic changes in steroid synthesis and lipid metabolism, including free fatty acids and other bioactive lipids. Other important enrichments included changes in the citric acid cycle and 1-carbon metabolism pathways implicated in DNA methylation. Although the minority of changes were observed in bone and plasma (<20), increased p-cresol sulfate was increased >4 fold in plasma (the largest increase in all tissues), and pantothenate (vitamin B5) decreased >2-fold. The results suggest that HFD-mediated β-cell expansion is associated with complex, global metabolite changes. The finding could be a significant insight into Type 2 diabetes pathogenesis and potential novel drug targets.
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Yuvaraj, S., Monica Mendon, Asha Almeida, Mini Dhiman et Manju Girish. « Synthesis of novel bioactive pyrazolothiazoles ». Medicinal Chemistry Research 23, no 5 (31 octobre 2013) : 2667–75. http://dx.doi.org/10.1007/s00044-013-0825-8.

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Wang, Zhuo, et Chunngai Hui. « Contemporary advancements in the semi-synthesis of bioactive terpenoids and steroids ». Organic & ; Biomolecular Chemistry 19, no 17 (2021) : 3791–812. http://dx.doi.org/10.1039/d1ob00448d.

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Litvinovskaya, R. P., S. V. Drach, M. E. Raiman et V. A. Khripach. « Novel synthesis of 2-isoxazolyl steroids ». Chemistry of Heterocyclic Compounds 43, no 5 (mai 2007) : 637–39. http://dx.doi.org/10.1007/s10593-007-0099-5.

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Seo, Youngwan, Jee H. Jung, Jung-Rae Rho, Jongheon Shin et Jun-Im Song. « Isolation of novel bioactive steroids from the soft coral Alcyonium gracillimum ». Tetrahedron 51, no 9 (février 1995) : 2497–506. http://dx.doi.org/10.1016/0040-4020(95)00014-y.

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Thèses sur le sujet "Synthesis Novel Bioactive Steroids"

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Usai, Igor. « Synthesis of novel bioactive doxycycline derivatives ». kostenfrei, 2008. http://www.opus.ub.uni-erlangen.de/opus/volltexte/2008/1082/.

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Gill, Iqbal Singh. « Enzymatic synthesis of short bioactive peptides in novel media ». Thesis, University of Reading, 1993. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.335913.

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Straniero, V. « DESIGN AND SYNTHESIS OF NOVEL BIOACTIVE PEPTIDES AND PEPTIDOMIMETICS ». Doctoral thesis, Università degli Studi di Milano, 2013. http://hdl.handle.net/2434/217536.

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Nowadays there’s a growing interest in biologically active peptides for the development of new therapeutics; however in some cases, they could not directly use as drugs, due to their inherent limitations, such as rapid metabolism and low oral activity. As a result, peptides are modified into peptidomimetics with specific characteristics, in a rational design. The present PhD project is focused on the synthesis of several peptides and peptidomimetics, structurally different and presenting individual features, properties, targets and pharmaceutical applications. In particular, two are the research studies we’ve developed during the three years, these are the design of novel Carnosine-like derivatives and of new Farnesyl Transferase Inhibitors (FTIs). Concerning the first topic, we investigated how Carnosine (β-alanyl-L-histidine) structural changes influence its role as scavenger of HNE (4-hydroxy-trans-2,3-nonenal) and other toxic aldehydes. For this reason we modified the carnosine structure firstly replacing the Hystidinil- portion with different aromatic system, secondly substituting the β-alanyl portion with ten different amino acids, chosen in order to cover exhaustively the available chemical space. Finally we rigidified the whole structure, inserting a 2-oxazolidinone; the entire compound underwent biological evaluation, testing their ability to quench HNE. As a result, some of the twenty dipeptides showed impressing scavenging activities and great selectivity towards toxic aldehydes, suggesting us that they can represent truly promising candidates for the design of improved carnosine derivatives. Regarding the second subject, we designed, synthesized and tested several peptidomimetics of the CAAX box, where CAAX is the sequence Cysteine-Valine-Isoleucine-Methionine, able to block the farnesylation of RAS proteins and therefore cell proliferation. The design started from a nanomolar range FTI, previously synthesized by our group, where the central dipeptide (AA) is replaced with a 4-amino-2-o-tolylbenzoyl spacer and the Cysteine (C) with the residue 2-amino-4-thiazolylacetyl. The synthesis of the novel FTIs followed two separate approaches; at first we kept the aromatic spacer and modified the N-terminal residue with other heterocycles; the unimproved antiproliferative activity suggested us to apply other kind of modification. Therefore we replaced the o-tolyl with six heteroaromatic residues, in addition the synthesized compounds presented, as N- terminal residue, the 2-amino-4-thiazolylacetyl itself or the 1,4-benzodioxan-2-ylmethyl or the 1,4-benzodioxan-2-ylformyl. In all the three series of compounds, the 2-thienyl, 1-naphtyl and the 3-furanyl derivatives showed the highest FTase inhibition, at low micromolar level. Taken together, our biological activities provide interesting results, confirming that peptides and peptidomimetics should be employed as therapeutics.
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Tinarelli, Alessandro <1975&gt. « Novel Methodologies for the Synthesis of Scaffolds for Bioactive Molecules ». Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2010. http://amsdottorato.unibo.it/2291/1/Tinarelli-Alessandro-tesi.pdf.

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Tinarelli, Alessandro <1975&gt. « Novel Methodologies for the Synthesis of Scaffolds for Bioactive Molecules ». Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2010. http://amsdottorato.unibo.it/2291/.

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Derudas, Marco. « Design, synthesis and biological evaluation of novel bioactive nucleosides and nucleotides ». Thesis, Cardiff University, 2009. http://orca.cf.ac.uk/55855/.

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At the present there are 36 approved antiviral drugs in the UK of which half are nucleoside analogues. However, the emergence of drug resistance and of new virus strains necessitates new drugs. In particular in this thesis, different nucleoside analogues were studied as potential antivirals. One of the major issues related to nucleoside analogues is the emergence of resistance due to a lack of bioactivation to the monophosphate form. To overcome this issue, the phosphoramidate ProTide technology can be applied. This strategy allows the delivery of the monophosphate form directly inside the cell. Bicyclic nucleoside analogues are a new class of anti-varicella zoster agents of which Cfl743 is the most potent anti-varicella zoster compounds reported to date. Its 5'-valyl derivative, FV100, is currently in phase II clinical trials. A series of derivatives to increase the activity and to investigate the mechanism of action of this new class of compound are reported. Moreover, attempts to improve the scale up synthesis of FV100 are described. Ribavirin is a broad spectrum antiviral drug. The application of the ProTide approach to this compound was not successful. Enzymatic and molecular modelling studies have been performed in order to understand the lack of activity. Acyclovir and its esters are currently the treatment of choice for herpes simplex and varicella-zoster infections. The application of the ProTide technology gave surprising results. In fact, these compounds have been found to be active against HIV, whilst ACV itself did not show any activity. Moreover, these compounds retained activity versus thymidine kinase deficient strains against which acyclovir lost activity. These striking results prompted us to investigate other different nucleoside analogues, through a virtual screening using reverse transcriptase, guanylate or adenylate kinase and human polymerase y. The selected nucleoside analogues from this study include: ganciclovir, penciclovir and their derivatives. ProTides of these are thus pursued.
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Tran, Wendy. « Synthesis of Bioactive Natural Products & ; Derivatives as Novel Anti-infectives ». Thesis, University of Sydney, 2020. https://hdl.handle.net/2123/23995.

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Throughout history natural products have served as a valuable resource for the treatment of various diseases. To this day, many of these ancient remedies and their derivatives are still in use. However, in recent years, antibiotic discovery has stagnated at a time where there has also been the alarming emergence of antibiotic resistance which threatens to undermine the effectiveness of existing therapies. As such, novel antimicrobial agents are urgently needed that possess unique mechanisms of action to those currently in use. A promising class of natural products that exhibit antimicrobial activity are the non-ribosomal peptides (NRPs). This thesis describes the synthesis and biological evaluation of a number of NRP-derived molecules with a view to discovering new antibiotic leads. Chapters 2 & 3 describe the design and synthesis of potent anti mycobacterial derivatives based on the sansanmycin natural product scaffold. This involved the development of a late stage diversification route, thereby providing a platform for expedient access to a diverse library of analogues. These analogues were subjected to biological evaluation, from which key structure activity relationships were elucidated for inhibition of the growth of Mycobacterium tuberculosis – the etiological agent of tuberculosis (TB). These studies ultimately led to the identification of a new lead compound which was further evaluated in two animal models of TB infection. Chapter 4 describes efforts towards the synthesis of the janthinocins, a class of NRPs with potent activity against Gram positive bacteria. The synthetic strategy relied on late stage, chemoselective transformations to install key functionalities namely, selective oxidation of tryptophan to afford β ketotryptophan and elimination of β methylcysteine to form dehydrobutyrine. A deoxy-variant of janthinocin B was successfully synthesised which was subjected to late stage oxidation to the parent natural product, albeit on a small scale.
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Chan, Lai Chun. « Synthesis of novel heterocyclic constraints as probes for peptide bioactive conformation ». Thesis, University of Bath, 1992. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.303487.

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Kilburn, John Paul. « Novel solid-phase synthesis strategies for the preparation of heterocycles and guanidines ». Thesis, Open University, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.247056.

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Brockbank, P. « Synthesis of biologically active steroids and a novel approach to a total synthesis of the natural product anthecularin ». Thesis, Queen's University Belfast, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.546014.

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Livres sur le sujet "Synthesis Novel Bioactive Steroids"

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Singh, Rajesh Kumar, dir. Key Heterocyclic Cores for Smart Anticancer Drug–Design Part I. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/97898150400741220101.

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This book provides an update on heterocyclic compounds that serve as key components of anti-cancer agents administered in pre-clinical settings. Many of the compounds highlighted in the book are being actively investigated for the bioactive properties against a range of cancer cell lines. There is potential for heterocyclic compounds to design agents that can target specific molecules to treat different types of cancers. Chapters are contributed by experts in pharmaceutical chemistry and are written to give a general overview of the topic to readers involved in all levels of research and decision-making in pharmaceutical chemistry and anti-cancer drug design. Part 1 of the book set covers these topics: - Heterocyclic anticancer compounds derived from natural sources with their mechanism of action - The role of terpenoids as anticancer compounds: an insight into prevention and treatment - Recent advances in synthesis and anticancer activity of benzothiazole hybrids as anticancer agents - Structure-activity relationship studies of novel hybrid quinoline and quinolone derivatives as anticancer agents - Tetrazoles: structure and activity relationship as anticancer agents - Progress in nitrogen and oxygen-based heterocyclic compounds for their anticancer activity: an update (2017-2020)
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Chapitres de livres sur le sujet "Synthesis Novel Bioactive Steroids"

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Lozano, José I., Georgia L. Carroll et R. Daniel Little. « Electroreductive Cyclization Reactions. Studies Directed Toward the Phorbol Esters and Bioactive Diterpenes ». Dans Novel Trends in Electroorganic Synthesis, 221–24. Tokyo : Springer Japan, 1998. http://dx.doi.org/10.1007/978-4-431-65924-2_67.

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Ley, Steven V. « Synthesis of Antifeedants for Insects : Novel Behaviour-Modifying Chemicals from Plants ». Dans Ciba Foundation Symposium 154 - Bioactive Compounds from Plants, 80–98. Chichester, UK : John Wiley & Sons, Ltd., 2007. http://dx.doi.org/10.1002/9780470514009.ch7.

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Suresh, Patil Shivprasad, Vinod Bhatt, Prithvi Pal Singh et Upendra Sharma. « Steroidal sapogenins from genus Trillium : Chemistry, synthesis, and opportunities in neuro-active steroids designing ». Dans Bioactive Natural Products, 67–95. Elsevier, 2021. http://dx.doi.org/10.1016/b978-0-12-819485-0.00004-9.

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Bhar, Shanta S., et M. M. V. Ramana. « Novel Domino Reactions for Synthesis of Bioactive Diterpenoids and Alkaloids ». Dans Bioactive Natural Products (Part O), 399–422. Elsevier, 2008. http://dx.doi.org/10.1016/s1572-5995(08)80010-5.

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Banik, Bimal. « Synthesis and Biological Studies of Novel β-Lactams ». Dans Chemistry and Pharmacology of Naturally Occurring Bioactive Compounds, 31–72. CRC Press, 2013. http://dx.doi.org/10.1201/b13867-4.

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« Synthesis and Biological Studies of Novel β-Lactams* ». Dans Chemistry and Pharmacology of Naturally Occurring Bioactive Compounds, 53–94. CRC Press, 2013. http://dx.doi.org/10.1201/b13867-7.

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Rodriguez, Jaime. « Polycyclic Amine Alkaloids (3-Alkylpiperidine Alkaloids) – Novel Marine Bioactive Compounds : Structure, Synthesis and Biochemical Aspects ». Dans Bioactive Natural Products (Part E), 573–681. Elsevier, 2000. http://dx.doi.org/10.1016/s1572-5995(00)80052-6.

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Brindha Devi, Parthiban, et Ridhanya Jeyaseelan. « Natural Medicinal Compounds from Marine Fungi towards Drug Discovery : A Review ». Dans Drug Design - Novel Advances in the Omics Field and Applications [Working Title]. IntechOpen, 2020. http://dx.doi.org/10.5772/intechopen.94137.

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Marine fungi are species of fungi which live in estuaries environment and marine environment. These species are found in common habitat. Marine fungi are rich in antimicrobial compounds such as anthrones, cephalosporins, peptides, steroids. These compounds which are derived mainly focused in the area of anti-inflammatory, anti-oxidant, anti-fungal, anti-microbial, anti-fouling activity. Bioactive terpene compounds are produced by marine fungi and marine derived fungi can produce sclerotides, trichoderins. Marine fungi have become the richest sources of biologically active metabolites and structurally novel in the marine environment. In a recent study the marine derived fungi dichotomomyces cejpii exhibits activity towards cannabinoid which is used to treat alzheimer dementia. Aspergillus unguis showed significant acetyl cholinesterase besides its anti-oxidant activity. These acts as a promising intent for discovery of pharmaceutically important metabolites like alkaloids, peptides. Computational (in silico) strategies have been developed and broadly applied to pharmacology advancement and testing. This review summarizes the bioactive compounds derived from marine fungi in accordance with the sources and their biological activities.
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Atta-ur-Rahman, M. Iqbal Choudhary et S. Ghulam Musharraf. « Microbial Transformation of Natural Products- A Tool for the Synthesis of Novel Analogues of Bioactive Substances ». Dans Frontiers in Natural Product Chemistry, 133–47. BENTHAM SCIENCE PUBLISHERS, 2009. http://dx.doi.org/10.2174/907752704410501010133.

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M. Iqbal Choudhary, Atta-ur-Rahman. « Microbial Transformation of Natural Products- A Tool for the Synthesis of Novel Analogues of Bioactive Substances ». Dans Frontiers in Natural Product Chemistry, 133–47. BENTHAM SCIENCE PUBLISHERS, 2012. http://dx.doi.org/10.2174/978160805212710501010133.

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Actes de conférences sur le sujet "Synthesis Novel Bioactive Steroids"

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Barbosa, Flavio A. R., Rômulo F. S. Canto et Antonio L. Braga. « Synthesis of novel 6-seleno-dihydropyrimidinones : Potentially bioactive compounds ». Dans 15th Brazilian Meeting on Organic Synthesis. São Paulo : Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-bmos2013_2013819222620.

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Gomha, Sobhi, Zeinab Muhammad, Mastoura Edrees, Hatem Gaber, Mohamed Amin et Islam Matar. « Synthesis Under Microwave Irradiation and Molecular Docking of Some Novel Bioactive Thiadiazoles ». Dans The 23rd International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland : MDPI, 2019. http://dx.doi.org/10.3390/ecsoc-23-06607.

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Vlaisavljevich, Eli, Logan P. Janka, Keat G. Ong et Rupak M. Rajachar. « Magnetoelastic Materials as Novel Bioactive Coatings for Bone Anchored Prostheses ». Dans ASME 2009 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2009. http://dx.doi.org/10.1115/sbc2009-206406.

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Enhanced fibroblast activity at the implant-soft tissue interface is a key concern to the long-term success of many implanted biomaterials. Uncontrolled fibrosis has been shown to dramatically decrease the stability, function, and lifespan of biomedical implants. Fibrosis, defined as the overgrowth of various tissues about the implant, is caused by the excess synthesis of extracellular matrix components, primarily collagen, and often leads to walling off and hardening (calcification) of tissues at the biomaterial interface (1). Fibrosis is currently a major deterrent to stable bone anchored prostheses. These bone anchored mounting systems are designed to surgically attach a prosthesis mounting post directly into a patient’s bone. The attached post protrudes from the bone through the overlying soft tissue of the amputated limb providing an external connection point for the prosthetic. Although the bone anchoring system dramatically improves prosthetic limb mechanical stability, uncontrolled fibrosis at the soft tissue-mounting post interface is a significant problem (2). The fibrosis caused from aberrant cellular growth leads to the formation of irregular skin folds that prevent proper sealing to the bone anchoring post and also serves as a site for opportunistic infection and failure of the prosthetic system.
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Holmes, Hal, Eli Vlaisavljevich, Ee Lim Tan, Keat G. Ong et Rupak M. Rajachar. « Magnetoelastic Materials as Novel Bioactive Coatings to Improve Integration of Percutaneous Implants ». Dans ASME 2011 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2011. http://dx.doi.org/10.1115/sbc2011-53308.

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Fibroblastic activity is an innate function of the host response. In the presence of many percutaneous biomedical implants, this activity becomes uncontrollable, resulting in significant fibrous overgrowth at the soft tissue-implant interface [1]. The aberrant cell growth associated with pathological fibrosis can lead to extensive remodeling and excessive synthesis of extracellular matrix (ECM) components, preventing proper integration [2]. Furthermore, these areas of irregular fibrotic activity can also serve as sites for opportunistic infection [3]. In brief, interfacial fibrosis is often responsible for the ultimate failure and increased risk of infection of percutaneous biomedical implants.
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Birichevskaya, L. L., M. A. Vinter, A. A. Doroshevich, M. А. Khancheuski, E. I. Kvasyuk et A. I. Zinchenko. « SYNTHESIS OF THE MODIFIED NUCLEOSIDE 8-BROMADENOSINE AND ITS PHOSPHOLIPID DERIVATIVE ». Dans SAKHAROV READINGS 2021 : ENVIRONMENTAL PROBLEMS OF THE XXI CENTURY. International Sakharov Environmental Institute of Belarusian State University, 2021. http://dx.doi.org/10.46646/sakh-2021-2-20-23.

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Modified nucleoside 8-bromoadenosine possessing high reactive capacity may serve as a basic compound for the synthesis of a large number of purine antimetabolites showing potentially therapeutic activities toward several tumor and viral diseases. In this study, 8-bromoadenosine was produced by a simple eco-friendly procedure following the treatment of nucleoside precursor adenosine with aqueous bromine solution. In the course of enzymatic transphosphatidylation reaction, the first synthesis of phospholipid derivative of the above-mentioned nucleoside -5‘-(1,2-dimyristoyl phosphatidyl)-8-bromoadenosine was accomplished. Novel compounds may presumably act as non-toxic progenitors of bioactive antimetabolites to be used in drug formulas.
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Bhushan, Indu. « Efficient media for high production of microbial lipase from Bacillus subtilis (BSK-L) using response surface methodology for enantiopure synthesis of drug molecules ». Dans 2nd International Scientific Conference "Plants and Microbes : the Future of Biotechnology". PLAMIC2020 Organizing committee, 2020. http://dx.doi.org/10.28983/plamic2020.044.

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Lipases are a multipurpose enzyme that holds a significant position in industrial applications due to its ability to catalyse a large number of reactions such as hydrolysis, esterification, interesterification, transesterification which makes it a potential candidate. It is also used for the separation of chiral drugs from the racemic mixture and this property of lipase is considered very important in pharmaceutical industries for the synthesis of enantiopure bioactive molecules. Assuming the tremendous importance of lipases, as stereoselective biocatalysts, in pharmaceuticals and various other commercial applications, industrial enzymologists have been forced to search for those microorganisms which are able to produce novel biocatalysts at reasonably high yield. In the present study microbial lipase was isolated from the water sample of pond at Katra, Jammu and Kashmir (India). This enzyme has shown wide specificity and higher enantioselectivity, which make it pharmaceutical important enzyme. To make it economical for industrial application, it was produced on cheap nutrient media using Response Surface Methodology and got maximum production. It was used for resolution of chiral drugs and the significant results obtained during the course of work shall have potential towards pharmaceutical industries.
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Dalli, Jesmond, Ana Rodriguez, Bernd Spur et Charles Serhan. « Structure elucidation and biological evaluations of sulfido-conjugated specialized pro-resolving mediators ». Dans 2022 AOCS Annual Meeting & Expo. American Oil Chemists' Society (AOCS), 2022. http://dx.doi.org/10.21748/mqgv6628.

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Inflammatory diseases are characterized by unabated inflammation that leads tissue destruction resulting in malaise. Whilst much is known on the mechanism that perpetuate inflammation, less is known about the molecules and pathways that coordinate the termination of inflammation and facilitate the repair and regeneration of damaged tissues. To evaluate the potential contribution of essential fatty acid-derived mediators in coordinating this life saving response we interrogated inflammatory exudates obtained following self-limited inflammatory challenge. Using radio-isotope tracking we found that the omega-3 fatty acid docosahexaenoic acid is utilized to produce novel bioactive molecules in these exudates. The structures of these molecules were elucidated using a range of physical techniques, demonstrating that these molecules were peptide lipid conjugated mediators and the stereochemistry of the functional groups was established using total organic synthesis. Investigations into their biosynthetic pathways demonstrated that the formation of their formation was initiated via the 14-lipoxygenation of DHA, that was then converted into an intermediate allylic epoxide and then conjugated to glutathione to yield the first mediator in the family which was coined as maresin conjugated in tissue regeneration (MCTR)1. This was then further converted to to 13-cysteinylglycinyl,14-hydroxy-docosahexaenoic acid (MCTR2) and 13-glycinyl,14-hydroxy-docosahexaenoic acid (MCTR3). Evaluation of the biological activities of these molecules demonstrated that they limited the recruitment of inflammatory cells to the sites of both sterile and infectious challenge. They reprogrammed biology towards a tissue protective phenotype and promoted the repair and regeneration of damaged tissues. Evaluation of the levels of these mediators in human peripheral blood demonstrated that the production of MCTR3 is significantly reduced in patients with rheumatoid arthritis that display signs of erosive joint disease. Together, these findings identify previously undescribed chemical signals that enhance host responses to limit inflammation, stimulate resolution of inflammation, and promote the restoration of function.
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Rapports d'organisations sur le sujet "Synthesis Novel Bioactive Steroids"

1

Hanson, Robert N. A Structure Based, Solid Phase Synthesis Approach to the Development of Novel Selective Estrogen Receptor Modulatory Steroids. Fort Belvoir, VA : Defense Technical Information Center, juillet 2001. http://dx.doi.org/10.21236/ada403350.

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Hanson, Robert N. A Structure Based, Solid-Phase Synthesis Approach to the Development of Novel Selective Estrogen Receptor Modulatory Steroids. Fort Belvoir, VA : Defense Technical Information Center, juillet 2002. http://dx.doi.org/10.21236/ada407782.

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Hanson, Robert. A Structure Based, Solid Phase Synthesis Approach to the Development of Novel Selective Estrogen Receptor Modulatory Steroids. Fort Belvoir, VA : Defense Technical Information Center, juin 2000. http://dx.doi.org/10.21236/ada383168.

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