Structure??Activity Relationship, Cytotoxicity and Mode of Action of 2??Ester??substituted 1, 5??Benzothiazepines as Potent Antifungal Agents

W Kang, X Du, L Wang, L Hu, Y Dong…

Index: Kang, Wang; Du, Xingqiong; Wang, Lanzhi; Hu, Lijuan; Dong, Yuhuan; Bian, Yanqing; Li, Yuan Chinese Journal of Chemistry, 2013 , vol. 31, # 10 p. 1305 - 1314

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Abstract

Abstract Our studies examined the structural features responsible for the antifungal activity of 2-ethoxycarbonyl-1, 5-benzothiazepine (7a). Three series of 1, 5-benzothiazepine derivatives were synthesized and screened for their antifungal activity. The results suggested that the ethoxycarbonyl group at the 2 position and the imine moiety on the seven- membered ring are essential for activity. The most potent of the synthesized analogues ( ...

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