Literature DB >> 20452209

Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Fa-Xiang Ding1, Hong C Shen, Larrisa C Wilsie, Mihajlo L Krsmanovic, Andrew K Taggart, Ning Ren, Tian-Quan Cai, Junying Wang, Xinchun Tong, Tom G Holt, Qing Chen, M Gerard Waters, Milton L Hammond, James R Tata, Steven L Colletti.   

Abstract

A series of pyrazolyl propionyl cyclohexenamides were discovered as full agonists for the high affinity niacin receptor GPR109A. The structure-activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20452209     DOI： 10.1016/j.bmcl.2010.04.013

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  2 in total

1.  One-pot synthesis of densely functionalized cyclic β-aminoesters containing four stereocenters, based on a Et3N-promoted pseudo five-component reaction.

Authors:  Juan Yao; Lanxiang Zhou; Chen Tan; Cunde Wang
Journal:  Mol Divers       Date:  2014-09-26       Impact factor: 2.943

Review 2.  G protein-coupled receptors for energy metabolites as new therapeutic targets.

Authors:  Clara C Blad; Cong Tang; Stefan Offermanns
Journal:  Nat Rev Drug Discov       Date:  2012-07-13       Impact factor: 84.694
  2 in total

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