Literature DB >> 15546720

CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.

Elfatih Elzein1, Prabha Ibrahim, Dmitry O Koltun, Ken Rehder, Kevin D Shenk, Timothy A Marquart, Bob Jiang, Xiaofen Li, Reina Natero, Yuan Li, Marie Nguyen, Suresh Kerwar, Nancy Chu, Daniel Soohoo, Jia Hao, Victoria Y Maydanik, David A Lustig, Dewan Zeng, Kwan Leung, Jeff A Zablocki.   

Abstract

New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50=380 nM rat mitochondria) with favorable PK properties (F=93%, t(1/2)=13.6h, dog).

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Year:  2004        PMID: 15546720     DOI: 10.1016/j.bmcl.2004.09.077

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


  2 in total

1.  Fatty-acid oxidation and calcium homeostasis are involved in the rescue of bupivacaine-induced cardiotoxicity by lipid emulsion in rats.

Authors:  Parisa Partownavid; Soban Umar; Jingyuan Li; Siamak Rahman; Mansoureh Eghbali
Journal:  Crit Care Med       Date:  2012-08       Impact factor: 7.598

Review 2.  Synthetic approaches and pharmacological activity of 1,3,4-oxadiazoles: a review of the literature from 2000-2012.

Authors:  Cledualdo Soares de Oliveira; Bruno Freitas Lira; José Maria Barbosa-Filho; Jorge Gonçalo Fernandez Lorenzo; Petrônio Filgueiras de Athayde-Filho
Journal:  Molecules       Date:  2012-08-27       Impact factor: 4.411

  2 in total

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