View source for BIOSIS / 2004:256580

AN   
     2004:256580  BIOSIS
DN   
     PREV200400256670
TI   
     Carbazates as potent inhibitors of hormone-sensitive lipase. 
AU   
     de Jong, Johannes C.; Sorensen, Lotte G.; Tornqvist, Hans; Jacobsen, Poul
     [Reprint Author]
CS   
     Medicinal Chemistry, Novo Nordisk A/S, Novo Nordisk Park, 2760, Maaloev,
     Denmark
     pjac@novonordisk.com
SO   
     Bioorganic & Medicinal Chemistry Letters, (5 April 2004) Vol. 14, No. 7,
     pp. 1741-1744. print. 
     CODEN: BMCLE8. ISSN: 0960-894X. 
DT   
     Article
LA   
     English
ED   
     Entered STN: 12 May 2004
     Last Updated on STN: 12 May 2004
AB   
     The central role of adipose tissue hormone-sensitive lipase in
     regulating fatty acid metabolism makes it a potential pharmacological
     target for the prevention of peripheral insulin resistance in obese,
     prediabetic and diabetic individuals.  The synthesis of a new series of
     carbazates is presented.  Modification of the phenolic 4-position in a
     series of 1,2,3,4-tetrahydroisoquinoline and morpholine derived
     carbazates, yielded inhibitors of the catalytic activity of this enzyme
     with nanomolar potency.
CC   
     Biochemistry studies - General   10060
     Biochemistry studies - Lipids   10066
     Enzymes - General and comparative studies: coenzymes   10802
     Pathology - Therapy   12512
     Metabolism - General metabolism and metabolic pathways   13002
     Metabolism - Metabolic disorders   13020
     Endocrine - Pancreas   17008
     Pharmacology - General   22002
IT   
     Major Concepts
        Enzymology (Biochemistry and Molecular Biophysics); Pharmacology
IT   
     Parts, Structures, & Systems of Organisms
        adipose tissue
IT   
     Diseases
        diabetes: endocrine disease/pancreas, metabolic disease, drug therapy
        Diabetes Mellitus (MeSH)
IT   
     Diseases
        obesity: nutritional disease
        Obesity (MeSH)
IT   
     Chemicals & Biochemicals
        1,2,3,4-tetrahydroisoquinoline; carbazates: enzyme inhibitor-drug;
        fatty acid: metabolism; hormone-sensitive lipase: inhibition; morphine
IT   
     Miscellaneous Descriptors
        peripheral insulin resistance
RN   
     91-21-4 (1,2,3,4-tetrahydroisoquinoline)
     9001-62-1 (hormone-sensitive lipase)
     57-27-2 (morphine)