Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator |
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| Authors: | Hassen Ratni Denise Blum-Kaelin Henrietta Dehmlow Peter Hartman Philippe Jablonski Raffaello Masciadri Cyrille Maugeais Angelique Patiny-Adam Narendra Panday Matthew Wright |
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| Institution: | F. Hoffmann-La Roche Ltd, Pharmaceuticals Division, Preclinical Research, CH-4070 Basel, Switzerland |
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| Abstract: | A series of tetrahydro-cyclopentab]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. |
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