Potent orally active inhibitors of angiotensin-converting enzyme (ACE).
1981; Pharmaceutical Society of Japan; Volume: 29; Issue: 8 Linguagem: Inglês
10.1248/cpb.29.2210
ISSN1347-5223
AutoresKatsuhiro Imaki, Shigeru Sakuyama, Takanori Okada, Masaaki Toda, Masaki Hayashi, Tsumoru Miyamoto, Akiyoshi Kawasaki, Tadao Okegawa,
Tópico(s)Chemical Reaction Mechanisms
Resumo1-[3-Mercaptoalkanoyl] pyroglutamic acids and 1-[3-mercaptoalkanoyl]-4-hetero (oxa, thia and aza) pyroglutamic acids were prepared and their inhibitory activities against angiotensin-converting enzyme (ACE) were examined. (2S)-1-[(2S)-3-Mercapto-2-methylpropanoyl] pyroglutamic acid 2 was found to be the most potent orally active inhibitor of ACE of rabbit lung among the derivatives synthesized in the present study and appeared to have great potential for use as an oral antihypertensive agent.
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