کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1363360 981510 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
چکیده انگلیسی

The SAR features have been further explored for (2-benzhydryl-4-phenyl-thiazol-5-yl)acetic acids as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. The introduction of a nitrogen or a methyl substituent in the benzhydrylic position offer two alternative drugable scaffolds attractive for unsymmetrically substituted derivatives. An imidazole analogue lacks activity due to formation of a favored coplanar intramolecular hydrogen bond. The pyrimidine derivative 18 represents a potent and selective compound that will be subject to continued investigations.

SAR data have been supported by key analogues of thiazoleacetic acids and modelling studies to arrive at potent and novel chemotypes of CRTH2 antagonists.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 5, 1 March 2010, Pages 1638–1641
نویسندگان
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