Synthesis and Antifungal Activity of 1, 5-Benzothiazepines Containing 1, 2, 3-Triazole

Abstract

Three kinds of 1, 5-benzothiazepines containing 1, 2, 3-triazole, 3-(1H-1, 2, 3-triazolyl)-4-aryl-2, 5-dihydro-1, 5-benzo-thiazepines (5a~5f), 3-(2H-1, 2, 3-triazolyl)-4-aryl-2, 3-dihydro-1, 5-benzothiazepines (6a~6f) and 3-(1H-1, 2, 3-triazolyl)-4-aryl-2, 3, 4, 5-tetrahydro-1, 5-benzothiazepines (7a~7f), were designed and synthesized. The synthesis conditions of intermediates and target products were studied. Two by-products were separated and their structures were determined. The antifungal activity test of the target products showed that compounds 5a~5f exhibited high inhibitory effects against fungi especially for Cryptococcus neoformans. The preliminary study on the structure-activity relationship of antifungal activity reveled that 1H-1, 2, 3-triazolyl and C=C double bond were the key function groups in the antifungal activity of 5a~5f.