Journal of medicinal chemistry

Antihypertensive agents: angiotensin converting enzyme inhibitors. 1-[3-(Acylthio)-3-aroylpropionyl]-L-prolines

FJ McEvoy, FM Lai, JD Albright

Index: McEvoy, Francis J.; Lai, Fong M.; Albright, J. Donald Journal of Medicinal Chemistry, 1983 , vol. 26, # 3 p. 381 - 392

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Citation Number: 26

Abstract

A series of l-[3-(acylthio)-3-aroylpropionyl]-~-proline derivatives was synthesized. A number of these compounds are potent angiotensin converting enzyme (ACE) inhibitors that lowered blood pressure in aorta-coarcted renal hypertensive rats. The most active derivatives are l-[3 (R)-(acetylthio)-3-substituted-benzoyl)-2 (S)-methyl-propionyll-prolines with an in vivo activity equivalent to SQ 14,225 (captopril). Structure-activity relationships are discussed. ...