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

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).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Elzein E,Ibrahim P,Koltun DO,Rehder K,Shenk KD,Marquart TA,Jiang B,Li X,Natero R,Li Y,Nguyen M,Kerwar S,Chu N,Soohoo D,Hao J,Maydanik VY,Lustig DA,Zeng D,Leung K,Zablocki JA

doi

10.1016/j.bmcl.2004.09.077

subject

Has Abstract

pub_date

2004-12-20 00:00:00

pages

6017-21

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01202-8

journal_volume

14

pub_type

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