Auswahl der wissenschaftlichen Literatur zum Thema „Bioactive heterocyclic compounds“

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Zeitschriftenartikel zum Thema "Bioactive heterocyclic compounds"

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Luna, Isadora Silva, Rayssa Marques Duarte da Cruz, Ryldene Marques Duarte da Cruz, Rodrigo Santos Aquino de Araújo und Francisco Jaime Bezerra Mendonça-Junior. „1,4-Dithiane-2,5-diol: A Versatile Synthon for the Synthesis of Sulfur-containing Heterocycles“. Current Organic Synthesis 15, Nr. 8 (17.12.2018): 1026–42. http://dx.doi.org/10.2174/1570179415666180821154551.

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Background: 1,4-Dithiane-2,5-diol (1,4-DTD) is the stable dimer of α-mercapto acetaldehyde. This commercially available ambidentade compound is characterized as having in its chemical structure one group that acts as an electrophile and another that acts as a nucleophile, this permits its use as versatile and efficient synthon in synthetic heterocycle procedures. Objective: The aim of this review is to present synthetic applications of 1,4-DTD in heterocyclic chemistry and their applicability to the synthesis of bioactive compounds. Conclusion: Gewald reactions to obtain C-4 and C-5 unsubstituted 2-amino-thiophene derivatives; sulfa- Michael/Henry and sulfa-Michael/aldol sequences to obtain polysubstituted tetrahydrothiophenes, and other heterocyclic reactions that allow synthesizing several functionalized sulfur-containing heterocycles such as thiazolidines, oxathiazinoles and thiazoles are presented and discussed. The use of such heterocyclics in subsequent reactions allows obtaining various bioactive compounds including the antiretroviral lamivudine which is one of the examples presented in this review.
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Adak, Laksmikanta, und Tubai Ghosh. „Recent Progress in Iron-Catalyzed Reactions Towards the Synthesis of Bioactive Five- and Six-Membered Heterocycles“. Current Organic Chemistry 24, Nr. 22 (18.12.2020): 2634–64. http://dx.doi.org/10.2174/1385272824999200714102103.

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Heterocyclic compounds are the largely diverse organic molecules and find prevalent applications in the fine chemical industry, medicinal chemistry and agricultural science. They are also among the most commonly bearing frameworks in numerous drugs and pharmaceutical substances. Therefore, the development of convenient, efficient and environmentally benign methods to produce various types of heterocyclic compounds is an attractive area of research. For the synthesis and functionalization of heterocycles, enormous achievements have been attributed over the past decades. Recently, ironcatalyzed reactions have accomplished a noteworthy development in the synthesis of heterocycles. This review highlights some remarkable achievements in the iron-catalyzed synthesis of heterocyclic compounds published in the last five years.
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Sharma, Praveen Kumar, Andleeb Amin und M. Kumar. „Synthetic Methods of Medicinally Important Heterocycles-thiazines: A Review“. Open Medicinal Chemistry Journal 14, Nr. 1 (14.09.2020): 71–82. http://dx.doi.org/10.2174/1874104502014010071.

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Heterocyclic compounds containing N and S atoms have unique properties so that they can be used as potential reactive materials in pharmacokinetic systems. In medicinal chemistry, the therapeutic applications of nitrogen sulphur heterocycles are well known. Especially, Thiazines attract the attention of chemists due to their great bioactive behavior. The present study is a review of the work carried out by the research community for the synthesis of novel, effective, medicinally important heterocyclic compounds-thiazines.
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Asif, Mohammad. „Biological Potential and Chemical Properties of Pyridine and Piperidine Fused Pyridazine Compounds: Pyridopyridazine a Versatile Nucleus“. Asian Journal of Chemistry and Pharmaceutical Sciences 1, Nr. 1 (21.11.2016): 29. http://dx.doi.org/10.18311/ajcps/2016/7693.

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Pyridopyridazine compounds are important nitrogen atom containing heterocyclic compounds due to their pharmacological versatility. This heterocycle system characterized a structural feature for different types of bioactive compounds that exhibiting various types of biological activities which make it an attractive scaffold for the design and development of new drug molecules. This article provided information about the pharmacological properties of pyridopyridazines derivatives.
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Sultan Alwan, Ensaf, und Rafat Milad Mohareb. „Synthesis of bioactive heterocyclic compounds using camphor“. Bulletin of the Chemical Society of Ethiopia 38, Nr. 4 (30.04.2024): 1069–76. http://dx.doi.org/10.4314/bcse.v38i4.20.

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The aim of the work was to synthesize novel heterocyclic compounds derived from camphor with antibacterial activity. The pyridazine, xanthene, pyranothiazole, pyridinothiazole, thiophene and pyrazole derivatives were produced from 4,11,11-trimethyl-9-phenyl-7-(2-phenylhydrazono)-3,4,5,6,7,9-hexahydro-1H-1,4-methanoxanthen-8(2H)-one (1). Thiophene derivatives 6a,b were produced according to the Gewald’s reaction for thiophene synthesis. On the other hand, pyranothiazol derivatives 8a,b were synthesized by the multicomponent reactions between xanthene derivative 5, benzaldehyde and ethylcyanoacetate or malononitrile in ethanol/triethylamine. Whereas, pyridinothiazole derivative 9 was produced in ethanol/ammonium acetate by the multicomponent reaction between xanthene derivative 5, benzaldehyde and malononitrile. The antibacterial activity of the synthesized compounds was evaluated against E. coli bacteria. All synthesized compounds showed moderate activity against E. coli bacteria. KEY WORDS: Anti-microbial, Camphor, Heterocyclic, Pyrazol-3(2H)-one, Thiazol-4(5H)-one, Thieno[3,2-d]thiazole, Xanthenes Bull. Chem. Soc. Ethiop. 2024, 38(4), 1069-1076. DOI: https://dx.doi.org/10.4314/bcse.v38i4.20
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Ge, Tony, und Jean-Christophe Cintrat. „Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery“. Pharmaceuticals 14, Nr. 12 (06.12.2021): 1275. http://dx.doi.org/10.3390/ph14121275.

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Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex molecules (polycyclic derivatives with two or more nitrogen atoms within the (fused) rings). In a constant quest for new chemical entities in drug discovery, a few novel heterocycles have emerged in recent years as promising building blocks for the obtainment of bioactive modulators. In this context, pyrrolotriazinones have attracted attention, and some show promising biological activities. Here, we offer an extensive review of pyrrolo[2,1-f][1,2,4]triazin-4(1H)-one and pyrrolo[1,2-d][1,2,4]triazin-4(3H)-one, describing their biological properties en route to drug discovery.
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Valdomir, Guillermo, María de los Ángeles Fernández, Irene Lagunes, Juan I. Padrón, Víctor S. Martín, José M. Padrón und Danilo Davyt. „Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells“. New Journal of Chemistry 42, Nr. 16 (2018): 13784–89. http://dx.doi.org/10.1039/c8nj02388c.

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Bassam A. Hassan, Hameedi N Nasera und Maitham M. Abdulridha. „Synthesis and antimicrobial evaluation of fused heterocyclic compound [1,2,4] triazolo [4,3-b][1,2,4,5] tetra zine“. International Journal of Research in Pharmaceutical Sciences 10, Nr. 2 (14.04.2019): 1254–58. http://dx.doi.org/10.26452/ijrps.v10i2.417.

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Nitrogen-containing, heterocycles, have special importance and vital, role in the discovery of effective bioactive, agents in the pharmaceutical, industry. The present article reports the synthesis of new fused, heterocycles triazolotetrazine by cyclo condensation, reaction as shown in scheme(1). The structures formula of synthesized compounds newly was evaluated by Ft-IR,1H-NMR spectrum, and C, H, N elemental analysis. Antimicrobial activity of triazolotetrazine studied against some pathogenic bacterial strains isolated from patients like Acinetobacter, Aeromonas, E. coli, Klebsiella, Staphylococcus, Streptococcus. Eventually, antibacterial of the fused heterocyclic compound was exhibited significant growth inhibition against some pathogenic bacteria which consider an important source of new antimicrobial compounds. The results, of such studies, are discussed in this paper.
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Akishina, E. A., und Е. А. Dikusar. „Chemical modification of different compounds with nitrogen-containing heterocycles“. Proceedings of the National Academy of Sciences of Belarus, Chemical Series 57, Nr. 3 (05.09.2021): 356–84. http://dx.doi.org/10.29235/1561-8331-2021-57-3-356-384.

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Heterocyclic compounds have an extremely important practical application, since many heterocycles are the basis of the most valuable medicinal substances, both natural (vitamins, enzymes, alkaloids, etc.) and synthetic biologically active compounds. The work mainly considers the most relevant directions for various purposes drugs search by modifying known bioactive natural, organoelement and framework compounds with 1,2-azole, oxazole, oxadiazole, thiazole, triazole, pyridine, pyrimidine heterocycles over the past 10 years. Chemical modification makes it possible to increase the water solubility of the compounds, which is important when choosing the pathways for the most rational drug introduction into the body, to reduce the toxicity of the corresponding substances, to increase the breadth of the therapeutic action, and also to give new valuable medicinal properties, thus significantly expanding their application in medicine and agriculture.
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Karan, Ram, Pooja Agarwal, Mukty Sinha und Neelima Mahato. „Recent Advances on Quinazoline Derivatives: A Potential Bioactive Scaffold in Medicinal Chemistry“. ChemEngineering 5, Nr. 4 (26.10.2021): 73. http://dx.doi.org/10.3390/chemengineering5040073.

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This paper intended to explore and discover recent therapeutic agents in the area of medicinal chemistry for the treatment of various diseases. Heterocyclic compounds represent an important group of biologically active compounds. In the last few years, heterocyclic compounds having quinazoline moiety have drawn immense attention owing to their significant biological activities. A diverse range of molecules having quinazoline moiety are reported to show a broad range of medicinal activities like antifungal, antiviral, antidiabetic, anticancer, anti-inflammatory, antibacterial, antioxidant and other activities. This study accelerates the designing process to generate a greater number of biologically active candidates.
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Dissertationen zum Thema "Bioactive heterocyclic compounds"

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Mojally, Mariam. „DNA binding studies of fluorinated bioactive heterocyclic compounds“. Thesis, Loughborough University, 2015. https://dspace.lboro.ac.uk/2134/16732.

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Fluorinated heterocyclic compounds have drug like properties and possess a valuable biological activity due to their rigid chemical structures and the high solubility profile. Novel fluorinated heteroarenes have been synthesised by SNAr reaction of a range of fluorinated arenes including pentafluoropyridine, hexafluorobenzene and pentafluorotoluene to introduce a range of groups specially nitriles, benzimidazole, carbazole and benzimidazole. A number of cyclization reactions have been investigated with the aim of forming polycyclic structures that could act as DNA intercalators. The synthesised compounds have been characterized by elemental analysis, IR, 1H and 19F NMR spectroscopy and single crystal analysis. These compounds have been screened for their biological activities including DNA thermal denaturation assay, UV-Visible spectroscopy, fluorescence spectroscopy, X-ray co-crystallization and antimicrobial activity study. Some of the compounds showed potential DNA bonding activity in particular the carbazole derivatives.
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Dey, Sourav. „Synthesis of bioactive organic heterocyclic compounds using novel catalysts“. Thesis, University of North Bengal, 2022. http://ir.nbu.ac.in/handle/123456789/5160.

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Trippier, Paul Charles. „Synthesis of highly substituted heterocycles : the oxazolomycins“. Thesis, University of Oxford, 2006. http://ora.ox.ac.uk/objects/uuid:b758987c-7a0c-4c1b-982c-61b4d383680a.

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This thesis is concerned with studies towards the total synthesis of a class of natural products - the oxazolomycins. Attention was focused on the left-hand side triene fragment and right-hand side lactam heterocyclic system. This thesis describes the synthesis of a racemic terminal phenyl analogue of oxazolomycin A and C, possessing the left-hand side triene geometry as required. A novel truncated pyridine analogue is also described. The molecules represent a racemic total synthesis of analogues of phthoxazolin A and inthomycins B and C. The synthesis is based upon a crucial Stille cross-coupling reaction between stannane and diene iodide fragments. The stannane fragment was synthesised using literature precedented methods and the vinyl halide prepared using a highly stereoselective Wittig, Takai homologation or Stork reaction leading to a variety of ratios of mixtures of Z, E and E, E diene halides. These investigations led to the availability of 1:1, 3:1 and 1:3 mixtures of Z, Z, E : Z, E, E left hand side triene fragments possessing the required stereochemistries for oxazolomycin A and C. Utilising existing methodology developed in the Moloney group, investigations were carried out towards construction of β-keto esters possessing terminal hydroxyl functions, suitable for diastereoselective aldol ring closure. Following extensive protecting group manipulation and N-acylation coupling optimisation, a TIPS protected β-keto acid, existing as predominantly the keto tautomer, was successfully coupled to an oxazolidine heterocycle. This N-acylated oxazolidine upon Dieckmann cyclisation would present an advanced intermediate of opposite configuration (Lserine is used here as a cheaper starting material for the construction of the oxazolidine instead of D-serine) to the oxazolomycin right-hand side.
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Mitra, Bijeta. „Development of new protocols towards construction of bioactive hetero cyclic compounds“. Thesis, University of North Bengal, 2021. http://ir.nbu.ac.in/handle/123456789/4368.

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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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Ferrazzano, Lucia <1989&gt. „Five-Membered Nitrogen Heterocycle Derivatives as Core Structures for the Synthesis of Bioactive Compounds Classes“. Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2017. http://amsdottorato.unibo.it/7956/1/PhD%20thesis%20Lucia%20Ferrazzano%20AMS%20dottorato.pdf.

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The research towards new cyclic isosteres of functional groups and the optimization of their synthesis have been one of the basis of this work. In particular, the attention was paid to three different heterocycles: isoxazolines, isoxazolidinones and 3,4-dehydro-beta-prolines. The synthetic protocols developed for them are based on the electrophylic properties of alkylidene acetoacetates, malonates, acetoacetamide esters and malonamides. Their preparation is found on Knöevenagel condensation and a microwaves-assisted protocol.For this last topic, two applications are microwave-assisted protocols for the Yonemitsu-type trimolecular condensation and for the one-pot two-steps synthesis of alkylidene acetoacetamide esters for the preparation of dehydropeptides. The reactivity towards indoles, amines and diprotected hydroxylamines is reported. 1,4-Michael addition of C- and N-nucleophyles to alpha,beta-unsaturated electrophyles is the ground for the synthesis of isoxazolines and isoxazolidinones, differently substituted. Then, the Luche-reduction of these unsaturated intermediates was investigated and the consequent enzymatic resolution for the enantioselective preparation of 3,4-dehydro-beta-prolines. Applications of the synthesized heterocycles in molecules with biological target are the synthesis of Linezolid analogues and peptidomimetic integrin ligands. Finally, the synthesis of red-shifted self-assembled nanoparticles as tools for bioimaging is reported.
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Frija, L. „Investigation of structural effects on the reactivity of heterocyclic bioactive compounds“. Doctoral thesis, 2008. http://hdl.handle.net/10400.1/856.

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Tese de dout., Química, Faculdade de Ciências e Tecnologia, Universidade do Algarve, 2008
In the course of this investigation, structural effects on the reactivity of a series of heterocyclic compounds, in particular tetrazole and benzisothiazole derivatives, submitted to different chemical environments, were explored. The photochemistry of several representative tetrazoles was considered in solution and for the compounds trapped in a rigid matrix of solidified argon at cryogenic temperatures. UV-excitation resulted in photofragmentation of tetrazoles with a wide range of exit channels. Important mechanistic questions concerning the photodecomposition of allyl-tetrazolyl derivatives in different solvents were answered, and new synthetic methodologies for the preparation of heterocyclic compounds, such as pyrimidinones or oxazines, from allyl-tetrazoles, were developed. For the matrix-isolated compounds, since the obtained fragments in general stay in the matrix cage where they are formed, no subsequent cross-reactions involving species resulting from photolysis of different reactant molecules can occur. This fact introduced a useful simplification for the interpretation of the reaction mechanisms. FTIR spectroscopy provided experimental frequencies and intensities of characteristic absorptions of the matrix-isolated chemical species, both for reagents and photoproducts. The analysis of experimental data was assisted by their direct comparison with the vibrational spectra theoretically calculated for the single molecule in vacuum. Spectroscopic characterization of a number of relatively unusual or highly reactive molecules, formed from photolysis of matrix-isolated tetrazoles, is presented for the first time. Novel tetrazolyl and benzisothiazolyl naphthylmethylic ethers were synthesized and the development of experimental conditions for their palladium-catalysed hydrogenolysis, using a hydrogen donor or molecular hydrogen, was carried out successfully. Structural effects on the reactivity of the heteroaromatic ethers were investigated. Furthermore, new benzisothiazole-tetrazolyl derivatives differing on the spacer-group used for linkage of the two heterocyclic systems were designed, produced and tested as multidentate ligands in coordination reactions with transition-metal complexes.
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Carvalho, Maria Solange Dantas de. „New heterocyclic bioactive fluorescent compounds: spectroscopic studies of DNA interactions and encapsulation in nanoliposomes“. Doctoral thesis, 2013. http://hdl.handle.net/1822/25580.

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Tese de doutoramento em Ciências (área de especialização em Química)
Spectroscopic studies (absorption and steady-state fluorescence) of potential antitumoral heteroaryl and heteroannulated indoles, benzothienopyran-1-ones, methyl 3-amino-6-heteroarylthieno[3,2-b]pyridine-2-carboxylates, tetracyclic thieno[3,2-b]pyridine derivatives and benzothienoquinolines, synthesized in our research group, were performed in solvent of different polarities. Generally, all the compounds presented a solvent sensitive emission with significant red-shifts in polar solvents, pointing out for their potential use as solvatochromic probes. The antitumoral potential of some of the compounds was evaluated by the growth inhibition of human tumor cell lines in collaboration with the Faculty of Pharmacy of the University of Porto. The spectroscopic properties of the compounds were also evaluated when incorporated in liposomes of neat lipids and lipid mixtures of different formulations, including, Egg-PC (egg yolk phosphatidylcholine), DPPC (dipalmitoyl phosphatidylcholine), DPPG (dipalmitoyl phosphatidylglycerol), DMPG (dimyristoyl phosphatidylglycerol), DOPE (dioleoyl phosphatidylethanolamine), DSPE-PEG (Distearoyl phosphatidylethanolamine-polyethylene glycol), DODAB (Dioctadecyldimethylammonium bromide) and cholesterol. Fluorescence steady-state anisotropy measurements allowed monitoring the location and behaviour of the compounds in the liposomes. In most cases, they showed to be located mainly in the hydrophobic region of the lipid bilayers, experiencing differences in fluidity between the rigid gel and the liquid-crystalline phases. These studies of the antitumoral compounds encapsulation were made having in mind future drug delivery applications. The mean size, size-distribution and zeta-potential of the liposomes incorporating the most promising antitumoral compounds, were determined by DLS (Dynamic Light Scattering). Almost all the liposomes with the incorporated compounds have shown diameters under 165nm and, with some formulations like DPPC:DMPG:DSPE-PEG (1:1:0.1), small diameters (below 100nm), low polydispersity and reasonable negative zeta-potential values were obtained for two of the methyl 3-amino-6- heteroarylthieno[3,2-b]pyridine-2-carboxylates studied. In order to evaluate the interaction with nucleic acids, the binding modes of the tetracyclic planar fluorescent thieno[3,2-b]pyridine derivatives and of the benzothienoquinolines to salmon sperm DNA and/or to synthetic double-stranded (ds) heteropolynucleotides were studied using spectroscopic methods which allowed the determination of intrinsic binding constants (Ki) and binding site sizes (n). Fluorescence quenching experiments with iodide ion were also performed in order to distinguish between the different binding modes of the compounds to the nucleic acids studied, since intercalated molecules are less accessible to anionic quenchers due to electrostatic repulsion with negatively charged nucleic acids. All the compounds interact with DNA and polynucleotides either by intercalation or groove binding. The latter seems to be the main type of interaction of these compounds with nucleic acids.
Foram realizados estudos espetroscópicos (absorção e fluorescência em estado estacionário) de heteroarilindoles e indoles heteroanelados, benzotienopiran-1-onas, 3-amino-6-heteroariltieno[3,2-b]piridina-2-carboxilatos de metilo, derivados tetracíclicos de tieno[3,2-b]piridinas e benzotienoquinolinas com potencial antitumoral, sintetizados no nosso grupo de investigação, em solventes de diferentes polaridades. De um modo geral, todos os compostos apresentaram uma emissão sensível ao solvente com significativos desvios para vermelho em meios polares, indicando a sua potencial utilização como sondas solvatocrómicas. O potencial antitumoral de alguns dos compostos foi avaliado através da inibição do crescimento de linhas celulares tumorais humanas em colaboração com a Faculdade de Farmácia da Universidade do Porto. As propriedades espetroscópicas foram também avaliadas para os compostos incorporados em lipossomas de lípidos puros e misturas lipídicas de diferentes formulações, incluindo, Egg-PC (fosfatidilcolina do ovo), DPPC (dipalmitoilfosfatidilcolina), DPPG (dipalmitoilfosfatidilglicerol), DMPG (dimiristoilfosfatidilglicerol), DOPE (dioleoilfosfatidiletanolamina), DSPE-PEG (Distearoil fosfatidiletanolamina-polietilenoglicol), DODAB (Brometo de dioctadecildimetilamónio) e colesterol. Medidas de anisotropia de fluorescência em estado estacionário permitiram monitorizar a localização dos compostos nos lipossomas. Na maioria dos casos, os compostos mostraram estar localizados maioritariamente na região hidrofóbica da bicamada lipídica, sentindo diferenças de fluidez entre a fase-gel e a fase líquidocristalina dos lípidos. Estes estudos de encapsulação dos compostos antitumorais foram realizados tendo em vista aplicações futuras de libertação de fármacos. O tamanho médio, distribuição de tamanhos e potencial-zeta dos lipossomas incorporando os compostos antitumorais mais promissores foram avaliados através de medidas de DLS (Difusão de Luz Dinâmica). A maioria dos lipossomas mostrou possuir diâmetros menores que 165nm e, algumas formulações como DPPC:DMPG:DSPE-PEG (1:1:0.1), exibiram tamanhos menores que 100nm e baixa polidispersividade. Valores de potencial-zeta razoavelmente negativos foram obtidos para dois dos 3-amino-6- heteroariltieno[3,2-b]piridina-2-carboxilatos de metilo estudados. Para avaliar a interação com os ácidos nucleicos, os modos de ligação dos derivados tetracíclicos fluorescentes planares de tieno[3,2-b]piridinas e de benzotienoquinolinas ao DNA de esperma de salmão e heteropolinucleótidos sintéticos de cadeia dupla, foram estudados usando métodos espetroscópicos que permitiram a determinação das constantes de ligação (Ki) e tamanho dos sítios de ligação (n). Medidas de inibição de fluorescência pelo ião iodeto foram também realizadas para distinguir entre os diferentes modos de ligação dos compostos aos ácidos nucleicos estudados, uma vez que as moléculas intercaladas estão menos acessíveis a inibidores aniónicos devido às repulsões eletrostáticas com os ácidos nucleicos carregados negativamente. Todos os compostos interatuam com o DNA e polinucleótidos ou por intercalação, ou por ligação nos sulcos (grooves). Este modo de ligação parece ser o tipo de interação predominante dos compostos com os ácidos nucleicos.
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Krishnan, Anand. „Synthesis of Bioactive Nitrogen Heterocycles and Functionalized Nanomaterials for Biological and Catalytic Applications“. Thesis, 2015. http://hdl.handle.net/10321/1181.

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Submitted in fulfillment of the requirements of the Degree of Doctor of Technology: Chemistry,Durban University of Technology, 2014.
Aromatic heterocycles are highly important structural units found in a large number of biologically active natural compounds, pharmaceuticals and catalytic compounds. They have a crucial role in organic syntheses, which results in the generation of high value products. Among heterocycles, those containing nitrogen are the most indispensable structural motifs and are widely used against dreaded diseases such as Malaria, TB, HIV/AIDS and Cancer. The inclusion of highly electronegative atoms such as fluorine in these organic molecules render them very reactive towards proteins. Furthermore these molecules exhibit strong interactions with surfaces of quantum range particles of elemental gold. Various approaches for the synthesis of novel gold nanoparticles linked to potent bioactive molecules are documented and their application as drug delivery systems are of immense value to human health. Also many chemical and physical methods are available for the synthesis of gold, silver and palladium nanoparticles however these methods are usually laborious and produce toxic by-products. The green approach is to use plant extracts to synthesise various size and shape nanoparticles which could be used in biological and catalytic systems. A simple one-pot two component and three component reaction using formyl quinoline, 2-aminothiophenol, thiosemicarbazone and trifluoromethylbenzaldehyde as a reactant to synthesise quinoline, pyridine and pyran based bioactive small molecules; these products are a quinoline type bearing a benzothiazole moiety, quinoline thio semicarbazone ligand, fluorine substituted dihydro pyridine, fluorine substituted dihydropyran and fluorine substituted pyridine derivatives. In total, fifteen compounds were synthesized eleven of which were novel; all compounds were characterized by spectroscopic techniques. In vitro anti-bacterial activities of the synthesized compounds were investigated against a representative panel of pathogenic strains. Compounds 6, 7, 8, 11 and 13 exhibited excellent anti-bacterial activity compared with first line drugs. Potent p53–MDM2 interaction inhibitors 2-thio-1,2-dihydroquinoline-3-carbaldehyde thiosemicarbazone and fluorine substituted new pyridine scaffold were successfully identified by structure-based design. An efficient one-pot four component route to the synthesis of trifluorinated pyrrolophenanthroline and fluoroquinoline pyrrolophenanthrolines was designed. In this reaction 1-butyl-2,3-dimethylimidazolium tetrafluoroborate ionic liquid (DMTIL) was used as a reaction medium; no catalyst was required. The structure of the pyrrolophenanthrolines was deduced by IR and NMR analysis. These compounds were studied with Bovine Serum Albumin (BSA) through molecular docking. Hydrophopic, electrostatic and hydrogen bonding interaction played a crucial role in the binding to sub domain of BSA. Interaction studies of DMTIL with BSA by emission, absorption, synchronous fluorescence, circular dichroism (CD) and three dimensional emission (3D) spectroscopic techniques were under taken. The results from emission titration experiments revealed the existence of a strong interaction between BSA and DMTIL ionic liquid. It showed that compounds with lesser number of hydrogen bonds are found to be more active which is attributed to hydrophobic interaction and electrostatic interaction which also played a vital role in DMTIL binding to sub domain IB of BSA. A novel copper-loaded boron nitride nanosheet (Cu/BN) catalyst was prepared and fully characterized. It was used as an efficient and chemoselective catalysts for the synthesis of α-aminophosphonates by the Kabachnik-Fields reaction; twenty one α-aminophosphonates were synthesised. The enhanced catalytic activity and product yield was attributed to the increase of surface acidity. Overall, this methodology offered competitive advantages such as recyclability of the catalyst without further purification or without using additives or cofactors, low catalyst loading, broad substrate applicability and high yields. The application of this new nanocatalyst in organic synthesis will provide a novel pathway for the synthesis of pharmaceutically important compounds. Gold nanoparticle surfaces were modified with self-assembled monolayers of important thiol and disulfide bioactive molecules since considerable interest is due to their potential application as anti-cancer agents. Herein, a carbazole was conjugated to lipoic acid by using an amide coupling catalyst HBTU and DIEA reaction. The structure of the carbazole thio octanic acid (CTN) was identified by IR and NMR. CTN was attached to the gold nanoparticles surface and the capping behaviour was characterized by UV-vis spectroscopy, TEM, DLS and FTIR. The cytotoxicity of CTNAuNPs on A549 cell lines was determined using the MTT assay. The results suggest CTN and CTNAuNPs possess anti-proliferative properties in the cancerous A549 cells. Furthermore a dual thiol ligand was synthesized by using equimolar 4-aminothiophenol (4-ATP) and amino oxadiazole thiol (AXT). This dual ligand was attached to the gold nanoparticles surface (DTAu) and the capping behaviour was characterized by UV-vis spectroscopy, TEM, DLS and FTIR. The cytotoxicity of DTAu on A549 cell lines was determined using the MTT assay. The results suggest dual ligands (4-ATP, AXT) and DTAu possess anti-proliferative properties in the cancerous A549 cells. South African indigenous plants and agroforestry waste were also used in the synthesis of silver, gold and palladium nanoparticles (NPs). Green protocols such as the use of environmentally benign solvents and non-hazardous reagents were an added advantage to physical and chemical means. Furthermore these reactions were rapid and the size and shape of the NPs could be manipulated by choosing the correct medium. The formulation of natural medicinal compounds capped onto NPs was assessed for their anti-cancer activity, in A549 lung cancer line, and catalytic reduction of dyes and nitrobenzene derivatives were studied. These NPs displayed: Significant cytotoxicity to lung cancer cells with minimal effect on normal healthy cells. Outstanding catalytic reduction of pharmaceutical and textile waste effluents such as dyes and nitro aromatic compounds. In addition, palladium nanoparticles containing capped Moringa olifera compounds were used effectively in the Suzuki coupling reaction of iodobenzene and phenylboronic acid. The reaction was rapid and was conducted in an aqueous medium.
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Bücher zum Thema "Bioactive heterocyclic compounds"

1

Eguchi, Shoji. Bioactive heterocycles. Herausgegeben von Eguchi Shoji. Berlin: Springer, 2006.

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Khan, Mahmud Tareq Hassan. Bioactive Heterocycles IV. Berlin, Heidelberg: Springer-Verlag Berlin Heidelberg, 2007.

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Khan, Mahmud Tareq Hassan. Bioactive Heterocycles III. Berlin, Heidelberg: Springer-Verlag Berlin Heidelberg, 2007.

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Khan, Mahmud Tareq Hassan. Bioactive Heterocycles V. Berlin, Heidelberg: Springer-Verlag Berlin Heidelberg, 2007.

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Motohashi, Noboru. Bioactive Heterocycles VI: Flavonoids and Anthocyanins in Plants, and Latest Bioactive Heterocycles I. Berlin, Heidelberg: Springer-Verlag Berlin Heidelberg, 2008.

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Motohashi, Noboru. Bioactive Heterocycles VII: Flavonoids and Anthocyanins in Plants, and Latest Bioactive Heterocycles II. Berlin, Heidelberg: Springer Berlin Heidelberg, 2009.

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Lamberth, Clemens, und Jürgen Dinges, Hrsg. Bioactive Heterocyclic Compound Classes. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.

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Dinges, Jürgen, und Clemens Lamberth, Hrsg. Bioactive Heterocyclic Compound Classes. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664450.

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9

Bioactive Marine Heterocyclic Compounds. MDPI, 2021. http://dx.doi.org/10.3390/books978-3-0365-2753-6.

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10

Usami, Yoshihide. Bioactive Marine Heterocyclic Compounds. Mdpi AG, 2021.

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Buchteile zum Thema "Bioactive heterocyclic compounds"

1

Ata, Athar, und Samina Naz. „Synthesis of Bioactive Heterocyclic Compounds“. In Greener Synthesis of Organic Compounds, Drugs and Natural Products, 137–50. Boca Raton: CRC Press, 2022. http://dx.doi.org/10.1201/9781003089162-8.

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Wong-Paz, Jorge E., Sylvain Guyot, Juan C. Contreras-Esquivel, Pedro Aguilar-Zárate, Raúl Rodríguez-Herrera und Cristóbal N. Aguilar. „Separation of Coffee Pulp Bioactive Phenolic Compounds by MPLC Fractionation and Identification by HPLC-ESI-MS“. In Modern Green Chemistry and Heterocyclic Compounds, 217–28. Series statement: Innovations in physical chemistry: monographic series: Apple Academic Press, 2020. http://dx.doi.org/10.1201/9780367276942-9.

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Dandia, Anshu, Shyam L. Gupta und Shuchi Maheshwari. „Molecular Iodine: Mild, Green, and Nontoxic Lewis Acid Catalyst for the Synthesis of Heterocyclic Compounds“. In Green Chemistry: Synthesis of Bioactive Heterocycles, 277–327. New Delhi: Springer India, 2014. http://dx.doi.org/10.1007/978-81-322-1850-0_10.

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Lamberth, Clemens, und Jürgen Dinges. „The Significance of Heterocycles for Pharmaceuticals and Agrochemicals*“. In Bioactive Heterocyclic Compound Classes, 1–20. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.ch1.

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Lamberth, Clemens. „Morpholine Fungicides for the Treatment of Powdery Mildew“. In Bioactive Heterocyclic Compound Classes, 119–27. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.ch10.

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Worthington, Paul. „Sterol Biosynthesis Inhibiting Triazole Fungicides“. In Bioactive Heterocyclic Compound Classes, 129–45. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.ch11.

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Lamberth, Clemens. „Methionine Biosynthesis-Inhibiting Anilinopyrimidine Fungicides“. In Bioactive Heterocyclic Compound Classes, 147–54. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.ch12.

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Lamberth, Clemens. „Phenylpyrrole Fungicides“. In Bioactive Heterocyclic Compound Classes, 155–62. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.ch13.

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Lamberth, Clemens. „Broad-Spectrum Fungicidally Active Pyrimidinyldioxy Strobilurins Inhibiting the Respiratory Chain“. In Bioactive Heterocyclic Compound Classes, 163–74. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.ch14.

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Walter, Harald. „Pyrazole Carboxamide Fungicides Inhibiting Succinate Dehydrogenase“. In Bioactive Heterocyclic Compound Classes, 175–93. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2012. http://dx.doi.org/10.1002/9783527664412.ch15.

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Konferenzberichte zum Thema "Bioactive heterocyclic compounds"

1

Verdes, Anastasia, Elena Gorincioi, Lucian Lupascu, Gheorghe Duca und Fliur Macaev. „Targeting the bioactive dihydropyrimidines by ecofriendly procedure of biginelli reaction: study case of monastrol“. In Scientific seminar with international participation "New frontiers in natural product chemistry". Institute of Chemistry, Republic of Moldova, 2023. http://dx.doi.org/10.19261/nfnpc.2023.ab24.

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Annotation:
Biologically active compounds decorated with dihydropyridine moiety are counted amongst the numerous broad-spectrum therapeutic agents that explain the increasing role of this scaffold in rational drug design [1]. The Biginelli reaction is a multicomponent reaction of aldehyde, (thio)urea, and ß-ketoester, involving Mannich reaction in the first step, which produces multifunctionalized 3,4-dihydropyrimidin-2-(1H)-ones and related heterocyclic compounds [2]. The attractiveness of this acid-catalyzed one-pot condensation reaction lies in the simplicity of grafting the substituent into the structure of the products, which can later be transformed into different functional groups that are required for subsequent syntheses. Monastrol, the most representative Biginelli adduct in anticancer drug development, proved to be a cell permeable molecule whose mechanism of action on cancer cells involves the selective inhibition of the motility of the mitotic motor enzyme kinesin Eg5 [3]. Thus the remarkable therapeutic and pharmacological potential of it maintains expressive interest of chemists, some green synthesis approaches being recently reported, as well [4,5]. In continuation of our research line [6], we herein report on a facile ecofriendly synthesis of (±)-M, based on the use of oxalic acid (20mol/%) as green catalyst instead of toxic Lewis acids. The proposed procedure also offers the advantage of shortening the reaction time twice, in comparison with the classic reaction, producing the racemic target compound in 60% yield, m.p. 182-184⁰C (crystallized from ethyl acetate), rep. 182-184⁰C [4,5]. The prepared (±)-monastrol has shown antifungal activity against Candida albicans and Saccharromyces cerevisiae at concentrations 8 times lower than reference antifungal agent Nystatin.
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