Benzothiophene and Its Derivatives as Promising Antimicrobial Agents: Characteristics synthesis and properties

Abstract

The increasing prevalence of antimicrobial resistance has created an urgent need for the development of novel antimicrobial agents with improved therapeutic efficacy. Benzothiophene, a biologically important sulfur-containing heterocyclic scaffold, has attracted considerable attention due to its diverse pharmacological activities and excellent synthetic versatility. In the present study, a series of novel benzothiophene derivatives (H1, H2, H4, and H5) were designed, synthesized, and evaluated for their antibacterial potential. The synthesized compounds were prepared through a multi-step synthetic approach involving the formation of a benzothiophene intermediate followed by functionalization with different substituted aniline derivatives. Structural characterization was carried out using FT-IR, LC-MS, and ¹H NMR spectroscopy, which confirmed the successful synthesis of the target compounds. The antibacterial activity was evaluated against Staphylococcus aureus (ATCC 12598) and Escherichia coli (ATCC 25922) using the broth microdilution method for determination of the minimum inhibitory concentration (MIC). Among the synthesized derivatives, compound H4 exhibited the most potent antibacterial activity, with MIC values of 4 µg/mL against S. aureus and 8 µg/mL against E. coli, whereas H2 showed moderate activity and H1 and H5 demonstrated comparatively lower antibacterial potency. These findings indicate that structural modification of the benzothiophene scaffold significantly influences antibacterial activity and highlights benzothiophene derivatives as promising candidates for the development of novel antimicrobial agents.