L-Phenylalanine-tethered Peptide Hydrazones of Chloro-based Thiophene-2-carboxamides: Design, Synthesis, and Anti-Microbial Studies

Abstract

In this article, we used thiophene-2-carboxamides as a starting material to synthesize a novel series of L-phenylalanine-tethered peptide hydrazones 6a–6o in three steps. The Broth Dilution Method was used to test the substance’ s antibacterial activity in vitro against a variety of bacteria and fungi. Compounds 6c, 6d, and 6g showed potent antibacterial activity against E. coli (MTCC 443) at 50 µg/mL; compounds 6a, 6b, 6g, and 6l were effective against P. aeruginosa (MTCC 1688); compound 6c was effective against S. aureus (MTCC 96); and compound 6a, 6c, and 6g were effective against S. pyogenes (MTCC 442). 6a, 6b, 6d, 6e, 6f, 6h–6l, 6n, and 6o all show considerable antifungal activity against C. albicans (MTCC 227) at 500 µg/mL. The effectiveness of synthesized compounds in a microbiological study was predicted using an in silico investigation of their pharmacokinetic properties (ADME).