THE DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF THE PEPTIDE DERIVATIVES CONTAINING GUANIDINE MOIETY WITH 5-CHLORO-THIOPHENE-2-CARBOXYLIC ACID CONJUGATES

Abstract

A new series of dipeptide derivatives with 5-chloro-thiophene-2-carboxylic acid conjugates have been designed and synthesized using solid-phase peptide synthesis. The synthesized dipeptide derivatives were characterized by using spectroscopic tools, like 1H and 13C NMR, IR, and mass and elemental analysis. Additionally, the obtained target dipeptide derivatives were evaluated for in vitro antimicrobial activity. The antibacterial activity of the target compounds was evaluated against four bacteria (two Gram-positive; Streptococcus pyogenes and Staphylococcus aureus, two Gram-negative; Escherichia coli and Pseudomonas aeruginosa). The screened analogs showed good antibacterial activity. Noteworthily, among them, Thiophene-Tyr-Arg-OH derivative exhibited excellent activity against Escherichia coli (MIC=15 µg/mL) as compared to standard drug ampicillin. The antifungal activity was evaluated against two fungi (Aspergillus niger and Candida albicans). The screened analogs also showed good antifungal activity.