RESUMO
One well-known multicomponent reaction that is helpful in the synthesis of dihydropyrimidinones (DHPMs), important molecules in organic synthesis and medicinal chemistry, is the Biginelli reaction. Because of their wide range of biological activities, DHPMs are regarded as essential chemicals. A great deal of research has been done in the last few decades to find ways to produce enantiomerically pure DHPMs because of their notable and focused target-oriented biological activities. In this reaction, numerous structural variants and catalysts have been employed in a range of solvents to yield an enormous number of Biginelli-type compounds. In the present review, the available catalysts in the literature including ionic liquids, Lewis acids, and organocatalysts for the Biginelli reaction and synthesis of a large number of asymmetric compounds since 2003 are summarized.
RESUMO
Schiff bases are one of the important classes of organic compounds containing imine or azomethine functional groups with potential biological applications in medicinal chemistry. Nowadays, these compounds have attracted the scientific community's attention due to their ability to act as ligands in the formation of stable metal complexes with significant biological activity. In this connection, we have designed and synthesized six novel thiophene-based organoltellurium (IV) complexes using a novel N-((5-methylthiophen-2-yl) methylene)-2-nitroaniline (5MTCONA) schiff base. These complexes underwent analytical investigation (TGA, Powder XRD, SEM, EDAX) as well as spectral analysis (FT-IR, NMR, Mass spectrometry, UV-Vis). The in-vitro pharmacological evaluation of these compounds has been carried out as antimicrobial and antioxidant agents. To further corroborate our findings, we have implemented computational analyses (Semi empirical PM3 method, Molecular Docking, and ADMET) of all the compounds with Spartan-14, Hex-8.0., Swiss ADME software. Precisely, our study integrates experimental and theoretical aspects, offering innovative insights in the field of pharmaceutical sciences.
Assuntos
Anti-Infecciosos , Complexos de Coordenação , Simulação de Acoplamento Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , Tiofenos/farmacologia , Anti-Infecciosos/farmacologia , Complexos de Coordenação/farmacologia , Complexos de Coordenação/química , Bases de Schiff/química , Ligantes , Testes de Sensibilidade Microbiana , Antibacterianos/farmacologiaRESUMO
Tuberculosis is a communicable disease which affects humans particularly the lungs and is transmitted mainly through air. Despite two decades of intensive research aimed at understanding and combating tuberculosis, persistent biological uncertainties continue to hinder progress. Nowadays, heterocyclic compounds have proven themselves in effective treatment of tuberculosis because of their wide range of biological and pharmacological activities. Antituberculosis or antimycobacterial agents encompass a broad array of compounds utilized singly or in conjunction to combat Mycobacterium infections, spanning from tuberculosis to leprosy. Here, we summarize the synthesis of various heterocyclic compounds which includes the greener synthetic route as well as use of nano compounds as catalyst along with their anti TB activities.
Assuntos
Antituberculosos , Compostos Heterocíclicos , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis , Antituberculosos/farmacologia , Antituberculosos/química , Antituberculosos/síntese química , Compostos Heterocíclicos/química , Compostos Heterocíclicos/farmacologia , Compostos Heterocíclicos/síntese química , Humanos , Mycobacterium tuberculosis/efeitos dos fármacos , Tuberculose/tratamento farmacológico , Estrutura MolecularRESUMO
Nowadays, the scientific community has focused on dealing with different kinds of diseases by exploring the chemistry of various heterocycles as novel drugs. In this connection, medicinal chemists identified carbonic anhydrases (CA) as one of the biologically active targets for curing various diseases. The widespread distribution of these enzymes and the high degree of homology shared by the different isoforms offer substantial challenges to discovering potential drugs. Medicinal and synthetic organic chemists have been continuously involved in developing CA inhibitors. This review explored the chemistry of different heterocycles as CA inhibitors using the last 11 years of published research work. It provides a pathway for young researchers to further explore the chemistry of a variety of synthetic as well as natural heterocycles as CA inhibitors.
Assuntos
Inibidores da Anidrase Carbônica , Anidrases Carbônicas , Química Farmacêutica , Compostos Heterocíclicos , Inibidores da Anidrase Carbônica/farmacologia , Inibidores da Anidrase Carbônica/síntese química , Inibidores da Anidrase Carbônica/química , Compostos Heterocíclicos/farmacologia , Compostos Heterocíclicos/química , Compostos Heterocíclicos/síntese química , Humanos , Anidrases Carbônicas/metabolismo , Anidrases Carbônicas/efeitos dos fármacos , Relação Estrutura-Atividade , Estrutura Molecular , AnimaisRESUMO
Double-headed warheads focusing on the pharmacological aspects as well as membrane permeability can contribute a lot to medicinal chemistry. Over the past few decades, a lot of research has been conducted on steroid-heterocycle conjugates as possible therapeutic agents against a variety of disorders. In the second half of the 20th century, successful research was conducted on cholesterol-based heterocyclic moieties. Keeping in view the biological significance of various triazoles, research on fusion with cholesterol has emerged. This review has been designed to explore the chemistry of cholesterol-based triazoles for the duration from 2010 to 2023 and their significance in medicinal chemistry.
RESUMO
Chalcone-derived isoxazole scaffolds remain the central focus due to their greater biological, clinical, and pharmacological properties. The present study reviews the synthesis of various chalcone derived - 5- membered isoxazoline and isoxazole scaffolds with the available literature until 2021.