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J Med Chem. 2001 Jul 19;44(15):2383-6.

Reversible carnitine palmitoyltransferase inhibitors with broad chemical diversity as potential antidiabetic agents.

Author information

1
Departments of Chemical Research, Endocrinology & Metabolism, and Analytical Research, Sigma Tau Pharmaceutical Industries S.p.A., Via Pontina Km 30.400, 00040 Pomezia, Italy. fabio.giannessi@sigma-tau.it

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.

PMID:
11448219
DOI:
10.1021/jm010889+
[Indexed for MEDLINE]

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