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A novel series of analogues based on 5-(1-(4-chloro-3-methoxyphenyl)piperidin-4-yl)-4-phenyl-2H-1,2,4-triazole-3(4H)-thione core have been synthesized and their potential as antibacterial, antifungal and antitubercular agents was examined. The structure-activity relationship (SAR) studies of these derivatives 5 (a-k) clearly indicate the vital role of lipophilicity as a major factor in enhancing the biological activity of these compounds. Among the compounds screened, 5a, 5c, 5d, 5j and 5k displayed significant activity against Mycobacterium tuberculosis H37Rv strain.

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A highly efficient protocol for the synthesis of diverse aryl (heteroaryl) substituted pyridyl oxadiazol‐2(3H)‐one analogues using Suzuki‐Miyaura cross‐coupling strategy under microwave enhanced conditions is developed. The method is found to be compatible with a wide range of aryl (heteroaryl) boronic acids.

An expedient, palladium-mediated cross-coupling approach to functionalize the benzimidazole-based core under microwave-assisted conditions has been developed and is described. This protocol, which incorporates appendage diversity on this potential scaffold, is found to be compatible with a wide range of electronicallyand sterically-divergent (hetero)aryl boronic acids. The use of the PdCl 2 /(SPhos) catalytic system allows the formation of a stable and highly active LPd(0) species which was found to be critical for the successful synthesis of these novel, pharmacologically-relevant molecules.

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