| Literature DB >> 11448219 |
F Giannessi1, P Chiodi, M Marzi, P Minetti, P Pessotto, F De Angelis, E Tassoni, R Conti, F Giorgi, M Mabilia, N Dell'Uomo, S Muck, M O Tinti, P Carminati, A Arduini.
Abstract
A series of carnitine related compounds of general formula XCH(2)CHZRCH(2)Y were evaluated as CPT I inhibitors in intact rat liver (L-CPT I) and heart mitochondria (M-CPT I). Derivative 27 (ZR = -HNSO(2)R, R = C(12), X = trimethylammonium, Y = carboxylate, (R) form) showed the highest activity (IC(50) = 0.7 microM) along with a good selectivity (M-CPT I/L-CPTI IC(50) ratio = 4.86). Diabetic db/db mice treated orally with 27 showed a significant reduction of serum glucose levels.Entities:
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Year: 2001 PMID： 11448219 DOI： 10.1021/jm010889+
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446