skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

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

Abstract

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:
; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ;  [1]
  1. (GSKNC)
Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
INDUSTRY
OSTI Identifier:
1025646
Resource Type:
Journal Article
Resource Relation:
Journal Name: Bioorg. Med. Chem. Lett.; Journal Volume: 21; Journal Issue: (4) ; 02, 2011
Country of Publication:
United States
Language:
ENGLISH
Subject:
59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES; BILE ACIDS; GLUCOSE; NAPHTHALENE; QUINOLINES

Citation Formats

Bass, Jonathan Y., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., Mills, Wendy Y., Navas, III, Frank, Parks, Derek J., Smalley, Jr., Terrence L., Spearing, Paul K., Todd, Dan, Williams, Shawn P., and Wisely, G. Bruce. Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene. United States: N. p., 2014. Web. doi:10.1016/j.bmcl.2010.12.089.
Bass, Jonathan Y., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., Mills, Wendy Y., Navas, III, Frank, Parks, Derek J., Smalley, Jr., Terrence L., Spearing, Paul K., Todd, Dan, Williams, Shawn P., & Wisely, G. Bruce. Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene. United States. doi:10.1016/j.bmcl.2010.12.089.
Bass, Jonathan Y., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., Mills, Wendy Y., Navas, III, Frank, Parks, Derek J., Smalley, Jr., Terrence L., Spearing, Paul K., Todd, Dan, Williams, Shawn P., and Wisely, G. Bruce. Wed . "Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene". United States. doi:10.1016/j.bmcl.2010.12.089.
@article{osti_1025646,
title = {Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene},
author = {Bass, Jonathan Y. and Caravella, Justin A. and Chen, Lihong and Creech, Katrina L. and Deaton, David N. and Madauss, Kevin P. and Marr, Harry B. and McFadyen, Robert B. and Miller, Aaron B. and Mills, Wendy Y. and Navas, III, Frank and Parks, Derek J. and Smalley, Jr., Terrence L. and Spearing, Paul K. and Todd, Dan and Williams, Shawn P. and Wisely, G. Bruce},
abstractNote = {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.},
doi = {10.1016/j.bmcl.2010.12.089},
journal = {Bioorg. Med. Chem. Lett.},
number = (4) ; 02, 2011,
volume = 21,
place = {United States},
year = {Wed Aug 13 00:00:00 EDT 2014},
month = {Wed Aug 13 00:00:00 EDT 2014}
}