کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362576 | 981490 | 2010 | 4 صفحه PDF | دانلود رایگان |
In this manuscript, we report the discovery of the substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors. 5c-(S) (SD-8381) was advanced into clinical studies due to its superior in vivo potency. The high plasma protein binding (>99% bound) of 5c-(S) has resulted in a surprisingly long human half life t1/2 = 360 h.
The design and synthesis of a series of potent and selective COX-2 inhibitors based on a benzopyran lead (1) is described. Our SAR studies allowed us to optimize this series resulting in the identification of clinical compound 5c-(S), which possesses superior in vivo efficacy in animal models of inflammation and pain.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 7155–7158