Synthesis of diverse heterocycles and identification of their potency as biological active agents

Abstract

quotA series of bis-triazole conjugates, N-aryl-2-(4-{[(1H-1,2,3-benzotriazol-1- newlineyl)oxy]methyl}-1H-1,2,3-triazol-1-yl)acetamides (6a-6j), have been synthesized via newlinecopper-catalyzed azide alkyne cycloaddition. Their antitubercular activity against the newlinehuman virulent H37Rv strain of Mycobacterium tuberculosis and anti-microbial action newlineagainst some Gram-positive and Gram-negative bacteria and fungal strains have been newlineevaluated. Enantiomerically amusing 2-(((1H-benzo[d][1,2,3]triazol-1- newlineyl)methyl)amino)-2-oxo-1-substitutedphenylethyl pyrazine-2-carboxylate (4a-4j), newlineproduced through a three-component passerine coupling reaction under GaCl3 as a newlinelewis acid-promoted conditions with diastereoselectivity ranging from moderate to newlinegood. The isolated library of compounds was screened for their biological activity newlineagainst Mycobacterium Tuberculosis H37Rv, and 4f featuring 4-F as substituent was newlinefound to be most active and synthesized the ten diverse scaffolds (5a-5j) by rightly newlineselecting the quinoline and pyrazine to articulate carboxamide derivatives in a singlestep process with maximum conversation in a shorter time through diversly studies of newlineUgi 4-CC reaction. Molecular docking studies against fms-like tyrosine kinase 3 (FLT3) newlineprovided well-clustered solutions for the binding modes of these molecules. They shed newlinelight on the key structural features governing the binding affinity. Synthesize Betti newlinebases (4a-4j) by a modified Betti reaction. We used 2-aminopyridin-3-ol, aromatic newlinealdehyde, and a naphthol system using greener media employing PEG-400 and newlinealumina as a prime active and highly selective catalyst. In vitro, anti-cancer screening newlineagainst NCI-60 call lines has shown exciting results. All synthesized compounds of the newlineseries were purified, identified, and characterized by MS, FT-IR, 1H NMR, and 13C newlineNMR.