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)