Synthesis and glycosidase inhibitory activities of nagstatin triazole analogs.

Recently, we have enatiospeciflcally synthesized nagstatin (1) and its analogs (for example, 2) having different configurations and functionalities and clarified the structure-activity relationships2 ~ 4). Herein, we describe the synthesis of the triazole analogs (3 and 4) having a triazole ring in place of an imidazole ring, and evaluate their glycosidase inhibitory activities to better understand the modeof action. In the synthesis of the triazole analogs, since two regioisomers (for example, ll and IT) would be possibly produced, AUG. 1996