Potent orally Active Inhibitors of Angiotensin-Converting Enzyme (ACE)

KATSUHIRO IMAKI; SHIGERU SAKUYAMA; TAKANORI OKADA; MASAAKI TODA; MASAKI HAYASHI; TSUMORU MIYAMOTO; AKIYOSHI KAWASAKI; TADAO OKEGAWA

doi:10.1248/cpb.29.2210

KATSUHIRO IMAKI, SHIGERU SAKUYAMA, TAKANORI OKADA, MASAAKI TODA, MASAKI HAYASHI, TSUMORU MIYAMOTO, AKIYOSHI KAWASAKI, TADAO OKEGAWA

Author information

Keywords: 1-[3-mercapto-2-methylpropanoyl] pyroglutamic acid

JOURNAL FREE ACCESS

1981 Volume 29 Issue 8 Pages 2210-2214

DOI https://doi.org/10.1248/cpb.29.2210

Details

Abstract

1-[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.

Corresponding author

Register with J-STAGE for free!