| Literature DB >> 19231176 |
Hassen Ratni1, Denise Blum-Kaelin, Henrietta Dehmlow, Peter Hartman, Philippe Jablonski, Raffaello Masciadri, Cyrille Maugeais, Angelique Patiny-Adam, Narendra Panday, Matthew Wright.
Abstract
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 LXRbeta versus LXRalpha 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.Entities:
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Year: 2009 PMID： 19231176 DOI： 10.1016/j.bmcl.2009.01.109
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823