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

Journal of Medicinal Chemistry

Volumn 44, Issue 15, 2001, Pages 2383-2386

  Giannessi, F ^a   Chiodi, P ^a   Marzi, M ^a   Minetti, P ^a   Pessotto, P ^a   De Angelis, F ^b   Tassoni, E ^a   Conti, R ^a   Giorgi, F ^a   Mabilia, M ^c   Dell'Uomo, N ^a   Muck, S ^a   Tinti, M O ^a   Carminati, P ^a   Arduini, A ^a  

^a Sigma Tau SpA   (Italy)

^b UNIVERSITY OF L'AQUILA   (Italy)

^c SIN Soluzioni Informatiche Sas   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; CARBOXYLIC ACID DERIVATIVE; CARNITINE PALMITOYLTRANSFERASE; CARNITINE PALMITOYLTRANSFERASE INHIBITOR; ENZYME INHIBITOR; TRIMETHYLAMMONIUM SALT DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DIABETES MELLITUS; DRUG SELECTIVITY; GLUCONEOGENESIS; GLUCOSE BLOOD LEVEL; HYPERGLYCEMIA; IC 50; NONHUMAN; RAT;

3-HYDROXYBUTYRIC ACID; ANIMALS; CARNITINE; CARNITINE O-PALMITOYLTRANSFERASE; ENZYME INHIBITORS; HYPOGLYCEMIC AGENTS; MITOCHONDRIA, HEART; MITOCHONDRIA, LIVER; RATS; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0035913058     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010889+     Document Type: Article

References (23)

1. Pathogenesis of NIDDM: A balanced overview
2. Relationships between plasma-free fatty acid concentration, endogenous glucose production, and fasting hyperglycemia in normal and noninsulin-dependent diabetic individuals
3. The mitochondrial carnitine palmitoyltransferase system. From concept to molecular analysis
4. Pyruvate carboxylase
5. Rationale and application of fatty acid oxidation inhibitors in treatment of diabetes mellitus
6. Carnitine Palmitoyltransferase: A Viable Target for the Treatment of NIDDM?
7. Chronic inhibition of fatty acid oxidation: New model of diastolic dysfunction
8. Hypoglycemic effects of a novel fatty acid oxidation inhibitor in rats and monkeys
9. Antidiabetic agents: A new class of reversible carnitine palmitoyltranferase I inhibitors
10. Antiketogenic and hypoglycemic effects of aminocarnitine and acylaminocarnitines
11. Stereoisomeric acylamidomorpholinium carnitine analogues: Selective inhibitors of carnitine palmitoyltransferase I and II
12. Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase
13. Stereospecific synthesis of (R)-aminocarnitine (Emeriamine) starting from (R)-carnitine via double inversion of configuration
14. Enantiomerically pure β, γ-epoxyesters from β-hydroxylactones: Synthesis of β-hydroxyesters and (-)-GABOB
15. Single step conversion of chiral carnitine and derivatives into (S)- and (R)-β-substituted-γbutyrolactones
16. New synthesis of (R, S)-carnitine chloride
17. The resolution of (±)-carnitine and the synthesis of acylearnitine
18. Regulation of ketone body metabolism
19. Development of hyperglycaemia and insulin resistance in conscious genetically diabetic (C57BL/KsJ db/db) mice
20. Isolation of a malonyl-CoA sensitive CPT/beta-oxidation enzyme complex from heart mitochondria
21. Improved methods to isolate and subfractionate rat liver mitochondria. Lipid composition of the inner and outer membrane