Literature DB >> 24618302

Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors.

Gang Zhou1, Pauline C Ting2, Grant Wishart2, Nicolas Zorn2, Robert G Aslanian2, Mingxiang Lin3, Michelle Smith4, Scott S Walker4, John Cook4, Margaret Van Heek4, Jean Lachowicz4.   

Abstract

Herein we report the design and synthesis of a series of novel bicyclic DGAT1 inhibitors with a carboxylic acid moiety. The optimization of the initial lead compound 7 based on in vitro and in vivo activity led to the discovery of potent indoline and quinoline classes of DGAT1 inhibitors. The structure-activity relationship studies of these novel series of bicyclic carboxylic acid derivatives as DGAT1 inhibitors are described.
Copyright © 2014 Elsevier Ltd. All rights reserved.

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Keywords:  Cyclohexanecarboxylic acid; DGAT1 inhibitor; Diacylglycerol acyltransferase inhibitor; Indoline; Quinoline; Triacylglyceride

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Year:  2014        PMID: 24618302     DOI: 10.1016/j.bmcl.2014.02.028

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


  2 in total

1.  Enabling Reductive C-N Cross-Coupling of Nitroalkanes and Boronic Acids by Steric Design of P(III)/P(V)═O Catalysts.

Authors:  Gen Li; Yuzuru Kanda; Seung Youn Hong; Alexander T Radosevich
Journal:  J Am Chem Soc       Date:  2022-05-02       Impact factor: 16.383

2.  Discovery of novel DGAT1 inhibitors by combination of machine learning methods, pharmacophore model and 3D-QSAR model.

Authors:  Hui Zhang; Chen Shen; Hong-Rui Zhang; Wen-Xuan Chen; Qing-Qing Luo; Lan Ding
Journal:  Mol Divers       Date:  2021-06-23       Impact factor: 3.364

  2 in total

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