کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1374173 981914 2009 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator
چکیده انگلیسی

A series of tetrahydro-cyclopenta[b]indoles modulating the activity of the liver-X-receptor (LXR) were derived from a high throughput screening hit. The potency and selectivity for LXRβ versus LXRα was improved. One compound, administered to wild-type mice modestly increased plasma HDL-cholesterol with no change in plasma triglycerides (TG) and reduced effects on liver TG content compared to T0901317. This novel series of LXR agonists shows promise to improve therapeutic efficacy with reduced potential to increase TG.

A novel series of selective LXRs modulator derived from a high throughput screening hit is reported.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 6, 15 March 2009, Pages 1654–1657
نویسندگان
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