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 ( ...