کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370936 | 981833 | 2011 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Two new series of EP4 antagonists based on naphthalene/quinoline scaffolds have been identified as part of our on-going efforts to develop treatments for inflammatory pain. One series contains an acidic sulfonylurea pharmacophore, whereas the other is a neutral amide. Both series show subnanomolar intrinsic binding potency towards the EP4 receptor, and excellent selectivity towards other prostanoid receptors. While the amide series generally displays poor pharmacokinetic parameters, the sulfonylureas exhibit greatly improved profile. MF-592, the optimal compound from the sulfonylurea series, has a desirable overall preclinical profile that suggests it is suitable for further development.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 3, 1 February 2011, Pages 1041–1046
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 3, 1 February 2011, Pages 1041–1046
نویسندگان
Jason D. Burch, Julie Farand, John Colucci, Claudio Sturino, Yves Ducharme, Richard W. Friesen, Jean-François Lévesque, Sébastien Gagné, Mark Wrona, Alex G. Therien, Marie-Claude Mathieu, Danielle Denis, Erika Vigneault, Daigen Xu, Patsy Clark,