Medicinal Chemistry

Synthesis and Antimicrobial Activity of Novel 3,7-Disubstituted 2H-1- Benzopyran-2-Ones

Abstract

Shailesh K, Devdutt C and Devi Prasad S

2H-1-benzopyran-2-one (Coumarin), an important oxygen heterocyclic scaffold, widely distributed throughout the plant kingdom, displayed a wide range of potential biological activities such as anti-microbial, anti-inflammatory and antioxidant activities. In this paper, we have synthesized a novel class of 3,7-disubstituted 2H-1-benzopyran- 2-one derivatives (3aa-3hb) bearing a basic ether side chain at C-7 and a substituted phenyl ring at C-3 of the coumarin ring. These compounds have been evaluated for anti-microbial (antibacterial/antifungal) activities. Some of the compounds 3ac, 3ae, 3bb, 3bc have shown significant anti-fungal activities against selective strains. Compound 3ae and 3bc with the MIC values of 1.56 μg/mL displayed better antifungal activity than fluconazole against Trichophyton mentagrophytes.