کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1372522 | 981871 | 2011 | 5 صفحه PDF | دانلود رایگان |
Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eyes where adverse effects were previously observed in rodents, representative systemically-distributed SCD1 inhibitors were converted into liver-targeting SCD1 inhibitors.
Novel and potent bicyclic heteroaryl SCD inhibitors were identified from optimization of a lead thiazole amide inhibitor, MF-152. In order to target the liver and to minimize systemic exposure to avoid skin and eye adverse events, representative systemically-distributed inhibitors were converted into liver-targeting SCD inhibitors.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 19, 1 October 2011, Pages 5692–5696