New Sulfhydryl Compounds with Potent Antihypertensive Activities

Abstract

(4R)-3-(Mercaptoacyl)-4-thiazolidinecarboxylic acids (III) were synthesized and their inhibitory activities against angiotensin-converting enzyme (ACE) were examined in vitro and in vivo. (4R)-3-[(2S)-3-Mercapto-2-methylpropanoyl]-4-thiazolidinecarboxylic acid (4a) was the most potent orally active inhibitor of ACE among the derivatives and its activity was almost same as that of (2S)-1-[(2S)-3-mercapto-2-methylpropanoyl] proline (8).