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
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator](/preview/png/1374173.png)
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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 6, 15 March 2009, Pages 1654–1657
نویسندگان
Hassen Ratni, Denise Blum-Kaelin, Henrietta Dehmlow, Peter Hartman, Philippe Jablonski, Raffaello Masciadri, Cyrille Maugeais, Angelique Patiny-Adam, Narendra Panday, Matthew Wright,