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

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

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
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Dec 20; Vol. 14 (24), pp. 6017-21.
Publication Year :
2004

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).

Details

Language :
English
ISSN :
0960-894X
Volume :
14
Issue :
24
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
15546720
Full Text :
https://doi.org/10.1016/j.bmcl.2004.09.077