Synthesis and Antimicrobial Activity of 5-(morpholinosulfonyl)isatin Derivatives Incorporating a Thiazole Moiety.

Abstract

This article describes the synthesis of novel 5-(morpholinosulfonyl)isatin derivatives having biologically active thiazole moiety were synthesized via 2 synthetic routes. The first route involved interaction of 5-(morpholino-sulfonyl) isatin with aminothiazole derivatives to give the Schiff's base derivatives (2, 3). The second route involved preparation of thiosemicarbazones (4-7) by treatment of 5-(morpholino- sulfonyl) isatin with thiosemicarbazides followed by cycloalkylation of the products with halogenated compounds to give the thiazole derivatives (8-19). Most of the synthesized compounds were screened against Gram (+), Gram (-) bacterial and fungi. The best gram positive activity was displayed by compounds 1, 13, 14, 15, 16 and 18 and the best gram negative bacteria was showed by compounds 1, 12, 13, 15, and 19, whereas compounds 1, 12, 13, 15, and 19 exhibited the best antifungal activity.