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)