Synthesis of thiophene derivatives and their anti-microbial, antioxidant, anticorrosion and anticancer activity

Abstract

Background: A new series of thiophene analogues was synthesized and checked for their in vitro antibacterial, antifungal, antioxidant, anticorrosion and anticancer activities. Results: A series of ethyl-2-(substituted benzylideneamino)-4,5,6,7-Tetrahydrobenzo[b]thiophene-3-carboxylate derivatives were synthesized by using Gewald synthesis and their structures were confirmed by FTIR, MS and 1H-NMR. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity against selected microbial species using tube dilution method, antiproliferative activity against human lung cancer cell line (A-549) by sulforhodamine B assay, antioxidant activity by using DPPH method and anticorrosion activity by gravimetric method. Conclusion: Antimicrobial screening results showed that compound S1 was the most potent antibacterial agent against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Salmonella typhi having MIC value 0.81 uM/ml and compound S4 also displayed excellent antifungal activity against both Candida albicans and Aspergillus niger (MIC = 0.91 uM/ml) when compared with cefadroxil (antibacterial) and fluconazole (antifungal) as standard drug. The antioxidant screening results indicated that compound S4 and S6 exhibited excellent antioxidant activity with IC50 values 48.45 and 45.33 respectively when compared with the ascorbic acid as standard drug. Anticorrosion screening results indicated that compound S7 showed more anticorrosion efficiency (97.90%) with low corrosion rate. Results of anticancer screening indicated that compound S8 showed effective cytotoxic activity against human lung cancer cell line (A-549) at dose of 10- 4 M when compared with adriamycin as standard.