Literature DB >> 20036121

2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.

Julianne A Hunt1, Silvia Gonzalez, Florida Kallashi, Milton L Hammond, James V Pivnichny, Xinchun Tong, Suoyu S Xu, Matt S Anderson, Ying Chen, Suzanne S Eveland, Qiu Guo, Sheryl A Hyland, Denise P Milot, Carl P Sparrow, Samuel D Wright, Peter J Sinclair.   

Abstract

The development of a series of 2-arylbenzoxazole alpha-alkoxyamide and beta-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated alpha-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole beta-alkoxyamine 4 showed a desirable combination of in vitro potency (IC(50)=151 nM) and oral bioavailability in the mouse. Copyright (c) 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID: 20036121     DOI: 10.1016/j.bmcl.2009.12.046

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


  2 in total

Review 1.  The role of ligand efficiency metrics in drug discovery.

Authors:  Andrew L Hopkins; György M Keserü; Paul D Leeson; David C Rees; Charles H Reynolds
Journal:  Nat Rev Drug Discov       Date:  2014-02       Impact factor: 84.694

2.  Docking and molecular dynamics study on the inhibitory activity of N, N-disubstituted-trifluoro-3-amino-2-propanols-based inhibitors of cholesteryl ester transfer protein.

Authors:  Bo-Liang Dong; Qing-Hua Liao; Jing Wei
Journal:  J Mol Model       Date:  2010-11-06       Impact factor: 1.810

  2 in total

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