The Synthesis and Angiotensin Converting Enzyme Inhibitory Activities of N-[(3-Substituted)aminocarbonyl]propanoyl-L-prolines
نویسنده
چکیده
Preparations of N-[3-(hetero)aryl-aminocarbonyl]propanoyl-L-proline derivatives 12, 13, 22 and 23 are described. A novel approach consists of fusing (80-100 °C) N-(hetero)aryl-succinimides (7, 8, 20, 21) with unprotected L-proline and imidazole in the presence of dimethylformamide. In vitro tests for angiotensin converting enzyme (ACE) inhibition showed that all N-(arylaminocarbonyl)-propanoyl-L-prolines (12, 13, 22 and 23) exhibit lower activity than captopril (1), their IC50's ranging from 2.5 X 10-4 to 3.3 X 10-3 M.
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