کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364311 981534 2006 12 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of heteroaryl sulfonamides as new EP1 receptor selective antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of heteroaryl sulfonamides as new EP1 receptor selective antagonists
چکیده انگلیسی

4-({2-[Isobutyl(phenylsulfonyl)amino]-5-(trifluoromethyl)phenoxy}methyl)benzoic acid (1) is a functional PGE2 antagonist selective for EP1 receptor subtype. Analogs of 1, in which the phenyl-sulfonyl moiety has been replaced with more hydrophilic heteroarylsulfonyl moieties, exhibited more optimized antagonist activity, while some of them showed in vivo antagonist activity. Structure–activity relationship (SAR) studies are also presented.

Heteroaryl sulfonamide derivatives 2–4 were identified as more potent and less lipophilic EP1 receptor antagonists than 1.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 19, 1 October 2006, Pages 6628–6639
نویسندگان
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