Synthesis of potential biologically active 1,2-benzothiazin-3-yl- quinazolin-4(3H)-ones

Abstract

A series of potential biologically active 2-(4-hydroxy-1,1-dioxido-2H-1,2- benzothiazin-3-yl)quinazolin-4(3H)-ones was synthesized in a straight forward manner by condensation of respective 4-hydroxy-1,2-benzothiazine-1,1-dioxides with anthranilamide followed by simple and high throughput cyclization of N-[2-(aminocarbonyl) phenyl]-4-hydroxy-1,2-benzothiazine-3-carboxamide-1,1- dioxides. All the synthesized compounds were subjected to preliminary evaluation for their biological activity against Gram positive and Gram negative bacteria. Some of the assayed compounds showed marked activity against Bacillus subtilis. © 2006 Pharmaceutical Society of Japan.