کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1374935 981928 2006 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Structure–activity relationship study between Ornithyl-Proline and Lysyl-Proline based tripeptidomimics as angiotensin-converting enzyme inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Structure–activity relationship study between Ornithyl-Proline and Lysyl-Proline based tripeptidomimics as angiotensin-converting enzyme inhibitors
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 8, 15 April 2006, Pages 2117–2121
نویسندگان
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