Inoue H, Konda M, Hashiyama T, Otsuka H, Watanabe A, Gaino M, Takahashi K, Date T, Okamura K, Takeda M, Narita H, Murata S, Odawara A, Sasaki H, Nagao T
Organic Chemistry Research Laboratory Tanabe Seiyaku Co., Ltd., Saitama Japan.
Chem Pharm Bull (Tokyo). 1997 Jun;45(6):1008-26. doi: 10.1248/cpb.45.1008.
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.
合成了在1,5-苯并硫氮杂䓬骨架的稠合苯环上被烷基、烷氧基、烷硫基、羟基或氨基取代的2,3-二氢-1,5-苯并硫氮杂䓬-4(5H)-酮，并研究了它们的血管舒张、抗高血压和血小板聚集抑制活性。选择(-)-顺式-3-乙酰氧基-5-[2-(二甲基氨基)乙基]-2,3-二氢-8-甲基-2-(4-甲基苯基)-1,5-苯并硫氮杂䓬-4(5H)-酮((-)-13e)作为血小板聚集的有效抑制剂进行进一步研究。
