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The Synthesis and Angiotensin Converting Enzyme Inhibitory Activities of N-[(3-Substituted)aminocarbonyl]propanoyl-L-prolines

Vitomir Šunjić ; Department of Organic Chemistry and Biochemistry »Ruder Boskovic« Institute, 41001 Zagreb, Yugoslavia
Šumski Šimaga ; Department of Organic Chemistry and Biochemistry »Ruder Boskovic« Institute, 41001 Zagreb, Yugoslavia
Ljubinka Vitale ; Department of Organic Chemistry and Biochemistry »Ruder Boskovic« Institute, 41001 Zagreb, Yugoslavia


Puni tekst: engleski pdf 7.158 Kb

str. 251-264

preuzimanja: 112

citiraj


Sažetak

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.

Ključne riječi

Hrčak ID:

194162

URI

https://hrcak.srce.hr/194162

Posjeta: 297 *