کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594372 | 981826 | 2012 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7)
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Design, synthesis and SAR analysis of the 5-chloro-4-(4-methoxyphenoxy)-2-(p-toly)pyridazin-3(2H)-one hit, identified through high-through-put screening (HTS) of the Molecular Libraries-Small Molecule Repository, led to the discovery of novel small molecule antagonists of NPBWR1 (GPR7). The lead molecule 5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy)pyridazin-3(2H)-one 1z (CYM50557) display submicromolar antagonist activity at the target receptor and high selectivity against a panel of therapeutically relevant off-targets. 1z may provide a pharmacological tool to probe the molecular basis of the in vivo physiological function and therapeutic utility of the target receptor in diverse disease areas including inflammatory pain and eating disorders.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7135-7141
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7135-7141
نویسندگان
Mariangela Urbano, Miguel Guerrero, Jian Zhao, Subash Velaparthi, S. Adrian Saldanha, Peter Chase, Zhiwei Wang, Olivier Civelli, Peter Hodder, Marie-Therese Schaeffer, Steven Brown, Hugh Rosen, Edward Roberts,