Thio-substd. (N)-propionyl-amino-acid derivs. - which are hypotensive angiotensin converting enzyme inhibitors

摘要

New N-thiopropionyl amino acid derivs. are cpds. of formula R4-S-CH2-CH-R3-CO-N-R2-CRR1-COOH (I) in which R and R1 are lower alkyl and R2 and R3 are H or lower alkyl, or R1 is linked with R or R2 so as to form a 5-membered ring; and R4 is H, lower alkanoyl or benzoyl. (I) are inhibitors of angiotensin converting enzyme and are useful in the treatment of hypertension, esp. angiotensin-induced hypertension. Specific cpds. (I) include 2- 3-(benzoylthio)propionamido -2-methylpropionic acid. In an example, this is prepd. by reacting alpha-aminoiosobutyric acid with 3-bromopropionyl chloride in the presence of NaOH, and reacting the product with thiobenzoic acid in the presence of K2CO3.