کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1363987 | 981525 | 2009 | 4 صفحه PDF | دانلود رایگان |
According to the docking studies and the analysis of a co-crystal structure of GW4064 with FXR, a series of 3-aryl heterocyclic isoxazole analogs were designed and synthesized. N-Oxide pyridine analog (7b) was identified as a promising FXR agonist with potent binding affinity and good efficacy, supporting our hypothesis that through an additional hydrogen bond interaction between the pyridine substituent of isoxazole analogs and Tyr373 and Ser336 of FXR, binding affinity and functional activity could be improved.
A series of 3-aryl heterocyclic isoxazole analogs were designed and synthesized, N-oxide pyridine analog (7b) was identified as a promising FXR agonist with potent binding affinity and good efficacy.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 9, 1 May 2009, Pages 2595–2598