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Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis
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2006 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 49, no 21, p. 6151-6154Article in journal (Refereed) Published
Abstract [en]

A structure-based approach was used to optimize our new class of quinoline LXR modulators leading to phenyl acetic acid substituted quinolines 15 and 16. Both compounds displayed good binding affinity for LXRâ and LXRR and were potent activators in LBD transactivation assays. The compounds also increased expression of ABCA1 and stimulated cholesterol efflux in THP-1 cells. Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knockout mouse model for lesions.

Place, publisher, year, edition, pages
2006. Vol. 49, no 21, p. 6151-6154
National Category
Pharmaceutical Sciences
Research subject
Biochemistry
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URN: urn:nbn:se:oru:diva-4127DOI: 10.1021/jm0609566PubMedID: 17034119OAI: oai:DiVA.org:oru-4127DiVA, id: diva2:138426
Note
Letter.Available from: 2007-11-06 Created: 2007-11-06 Last updated: 2018-01-13Bibliographically approved

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Enroth, Cristofer

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