Synthesis and Biological Evaluation of Alkyl, Alkoxy, Alkylthio, or Amino-Substituted 2, 3-Dihydro-1, 5-benzothiazepin-4(5H)-ones

Abstract

2, 3-Dihydro-1, 5-benzothiazepin-4(5H)-ones substituted with an alkyl, alkoxy, alkylthio, hydroxy, or amino group on the fused benzene ring of the 1, 5-benzothiazepine skeleton were synthesized and their vasodilating, antihypertensive, and platelet aggregation-inhibitory activities were investigated. (-)-cis-3-Acetoxy-5-[2-(dimethylamino)ethyl]-2, 3-dihydro-8-methyl-2-(4-methylphenyl)-1, 5-benzothiazepin-4(5H)-one ((-)-13e) was selected for further studies as a potent inhibitor of platelet aggregation.