Synthesis biological evaluation of alkyl, alkoxy, alkylthio, or amino-substituted 2,3-dihydro-1,5-benzothiazepin-4(5H)-ones.
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.
Inoue
H
H
Organic Chemistry Research Laboratory Tanabe Seiyaku Co., Ltd., Saitama Japan.
Konda
M
M
Hashiyama
T
T
Otsuka
H
H
Watanabe
A
A
Gaino
M
M
Takahashi
K
K
Date
T
T
Okamura
K
K
Takeda
M
M
Narita
H
H
Murata
S
S
Odawara
A
A
Sasaki
H
H
Nagao
T
T
D000478:Alkylation; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002560:Cerebrovascular Circulation / Q000187:drug effects; D003326:Coronary Circulation / Q000187:drug effects; D004110:Diltiazem / Q000031:analogs & derivatives* / Q000494:pharmacology; D004285:Dogs; D006168:Guinea Pigs; D006801:Humans; D008956:Models, Chemical; D008958:Models, Molecular; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011918:Rats, Inbred SHR; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology
D000959:Antihypertensive Agents; D010975:Platelet Aggregation Inhibitors; D014665:Vasodilator Agents; D004110:Diltiazem