Some Novel Chalcone Derivatives containing 5-Chloro Thiophene in a Base Structure: Synthesis, Characterization, in silico Study and Biological Evaluation

Abstract

A novel series of chalcone derivatives (4a-o) of N-(4-acetylphenyl)-5-chlorothiophene-2-carboxamide was synthesized by coupling it with different substituted aromatic aldehydes. Synthesized chalcones were characterized by IR, NMR and mass spectra. They were screened in vitro antibacterial activity against four bacterial cultures and antifungal activity against three fungal cultures by using broth-dilution method. The significant antibacterial activity with ≤ 50 μg/mL has been displayed by compounds 4b and 4n against E. coli (MTCC 443), compounds 4b, 4e, 4i, 4n and 4o against P. aeruginosa (MTCC 1688), compounds 4c and 4n against S. aureus (MTCC 96). In silico investigation was also carried out to predict pharmacokinetic properties (ADME) of synthesized chalcone derivatives.