REGIOSELECTIVE SYNTHESIS AND ANTIMICROBIAL SCREENING OF NOVEL S-ALKYL DERIVATIVES OF 5-(PYRIDIN-4-YL)-1,3,4-OXADIAZOLE-2-THIOL
Abstract
In medicinal chemistry, the molecular hybridization strategy—which entails merging two or more distinct bioactive pharmacophores into a single molecular entity—represents a highly effective approach to overcoming the challenges of drug-resistant pathogenic strains [1]. Both the pyridine ring (a core fragment of isoniazid) and the 1,3,4-oxadiazole heterocycle are well-recognized for their potent standalone antimicrobial and mycobacterial efficacies [2]. Consequently, structural modification at the exocyclic sulfur atom of the 5-(pyridin-4-yl)-1,3,4-oxadiazole-2-thiol scaffold, which inherently consolidates these two privileged nuclei, significantly calibrates the lipophilicity profile (log P) of the system, thereby enhancing the overall bioavailability and pharmacokinetic manageability of the potential therapeutic agent [3, 4].
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