کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374935 | 981928 | 2006 | 5 صفحه PDF | دانلود رایگان |

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′P1′ position was better suited to inhibit ACE, with propionic acid (C3) derived heterocyclics and unnatural amino acids.
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 designed and synthesized as possible angiotensin-converting enzyme (ACE) inhibitors.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 8, 15 April 2006, Pages 2117–2121