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Synthesis biological evaluation of alkyl, alkoxy, alkylthio, or amino-substituted
H Inoue1, M Konda, T Hashiyama
1Organic Chemistry Research Laboratory Tanabe Seiyaku Co., Ltd., Saitama Japan.
Chemical & Pharmaceutical Bulletin
|June 1, 1997
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-(di-methylamino) 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.