ABSTRACT
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.
Subject(s)
Carbonic Anhydrase Inhibitors , Carbonic Anhydrases , Chemistry, Pharmaceutical , Heterocyclic Compounds , Carbonic Anhydrase Inhibitors/pharmacology , Carbonic Anhydrase Inhibitors/chemical synthesis , Carbonic Anhydrase Inhibitors/chemistry , Heterocyclic Compounds/pharmacology , Heterocyclic Compounds/chemistry , Heterocyclic Compounds/chemical synthesis , Humans , Carbonic Anhydrases/metabolism , Carbonic Anhydrases/drug effects , Structure-Activity Relationship , Molecular Structure , AnimalsABSTRACT
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.
ABSTRACT
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.
Subject(s)
Antitubercular Agents , Heterocyclic Compounds , Microbial Sensitivity Tests , Mycobacterium tuberculosis , Antitubercular Agents/pharmacology , Antitubercular Agents/chemistry , Antitubercular Agents/chemical synthesis , Heterocyclic Compounds/chemistry , Heterocyclic Compounds/pharmacology , Heterocyclic Compounds/chemical synthesis , Humans , Mycobacterium tuberculosis/drug effects , Tuberculosis/drug therapy , Molecular StructureABSTRACT
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.
Subject(s)
Anti-Infective Agents , Coordination Complexes , Molecular Docking Simulation , Spectroscopy, Fourier Transform Infrared , Thiophenes/pharmacology , Anti-Infective Agents/pharmacology , Coordination Complexes/pharmacology , Coordination Complexes/chemistry , Schiff Bases/chemistry , Ligands , Microbial Sensitivity Tests , Anti-Bacterial Agents/pharmacologyABSTRACT
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.
