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Title: Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene

To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes.
Authors:
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  1. (GSKNC)
Publication Date:
OSTI Identifier:
1025646
Resource Type:
Journal Article
Resource Relation:
Journal Name: Bioorg. Med. Chem. Lett.; Journal Volume: 21; Journal Issue: (4) ; 02, 2011
Research Org:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Org:
INDUSTRY
Country of Publication:
United States
Language:
ENGLISH
Subject:
59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES; BILE ACIDS; GLUCOSE; NAPHTHALENE; QUINOLINES