Journal of Medicinal Chemistry p. 1984 - 1991 (1987)
Update date:2022-08-04
Yanagisawa, Hiroaki
Ishihara, Sadao
Ando, Akiko
Kanazaki, Takuro
Miyamoto, Shuichi
et al.
α-<6-<<(S)-1-(Ethoxycarbonyl)-3-phenylpropyl>amino>-5-oxoperhydro-1,4-thiazepin-4-yl>acetic acids (monoester monoacids) and their dicarboxylic acids having the hydrophobic substituents at the 2- or 3-position of the thiazepinone ring were prepared and assayed for angiotensin-converting enzyme (ACE) inhibitory activity.The dicarboxylic acids having the pseudoequatorial amino groups at the 6-position and the pseudoequatorial hydrophobic substituents at the 2- or 3-position of the chair conformation of the thiazepinone ring had potent in vitro inhibitory activity.The monoester monoacids having the hydrophobic substituents at the 2-position suppressed pressor response to angiotensin I for a longer duration than those having the substituents at the 3-position when administered orally.The structure-activity relationship was studied by conformational energy calculations of the thiazepinone ring.
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