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Aminocarnitine Ureidic Derivatives as Inhibitors of Carnitine Palmitoyltransferase I
Author(s) -
Tassoni Emanuela,
Conti Roberto,
Gallo Grazia,
Vincenti Silvia,
Dell'Uomo Natalina,
Mastrofrancesco Lucilla,
Ricciolini Rita,
Cabri Walter,
Carminati Paolo,
Giannessi Fabio
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900535
Subject(s) - chemistry , carnitine o palmitoyltransferase , carnitine , pharmacology , stereochemistry , biochemistry , combinatorial chemistry , enzyme , medicine , beta oxidation
Aminocarnitine ureidic derivatives were synthesized and evaluated as liver‐isoform‐selective carnitine palmitoyltransferase (CPT) I inhibitors. The most interesting molecule identified ( 3 ), the corresponding phosphonium analogue ( 4 ) showed improved efficacy in vitro and in vivo over the previously identified compound 1 (teglicar, ST1326).