Title of article :
Structure–activity relationship study between Ornithyl-Proline and Lysyl-Proline based tripeptidomimics as angiotensin-converting enzyme inhibitors
Author/Authors :
Mahesh Chand Pavar، نويسنده , , Kashif Hanif، نويسنده , , Amir Azam، نويسنده , , Sneh lata، نويسنده , , M.A. Qadar Pasha، نويسنده , , Santosh Pasha، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
Abstract :
A designed library of tripeptidomimics of Ornithyl-Proline (Orn-Pro) and Lysyl-Proline (Lys-Pro) conjugated with various unnatural amino acids and carboxylic acid derived heterocyclics was synthesized and screened for possible inhibitors of angiotensin-converting enzyme (ACE). Among the tripeptidomimics 10[MTP-Orn-Pro], 11[HTP-Orn-Pro], 14[TA-Orn-Pro] and 20[BPA-Orn-Pro] showed prominent inhibition with IC50 values in micromolar concentrations. Structure–activity relationship study indicated that C3 side chain of Orn as compared to C4 side chain of Lys at P1′ position was better suited to inhibit ACE, with propionic acid (C3) derived heterocyclics and unnatural amino acids.
Keywords :
ACE inhibitors , Unnatural amino acids , Carboxylic acid derived heterocyclics , Tripeptidomimics
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
