Carbazates as potent inhibitors of hormone-sensitive lipase
摘要:
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. (C) 2004 Elsevier Ltd. All rights reserved.
Carbamate triserine lactone receptors for anion recognition
摘要:
We have taken advantage of the ability of the cyclic triester of L-serine to organize ligand units appended to the three alpha-amine functionalities, as in enterobactin, a siderophore produced by enteric bacteria that binds ferric ion exceptionally well (K-f = 10(49)). As an extension of the preorganization concept, this work describes the preparation and characterization of carbamate triserine lactone receptors 1-6 and their ability to act as molecular receptors for anions. These receptors bind halides (F- >> Cl- > Br- > I-) with binding constants K in the range 21-7350 L mol(-1). (C) 2008 Elsevier Ltd. All rights reserved.
Compounds for treating disorders where a decreased level of plasma FFA is desired
申请人:——
公开号:US20020082254A1
公开(公告)日:2002-06-27
The present invention relates to novel compounds, compositions containing them, and their use for treating medical disorders where a decreased level of plasma free fatty acids (FFA) is desired.
REITER J.; PONGO L.; DVORTSAK P., J. HETEROCYCL. CHEM., 24,(1987) N 1, 127-142
作者:REITER J.、 PONGO L.、 DVORTSAK P.
DOI:——
日期:——
[EN] COMPOUNDS FOR TREATING DISORDERS WHERE A DECREASED LEVEL OF PLASMA FFA IS DESIRED<br/>[FR] COMPOSES DESTINES AU TRAITEMENT DE TROUBLES DANS LESQUELS UNE DIMINUTION DU NIVEAU D'AGL DU PLASMA EST VOULUE
申请人:NOVO NORDISK AS
公开号:WO2001087843A1
公开(公告)日:2001-11-22
The present invention relates to novel compounds of general formula (I), wherein A is a nitrogen containing ring systen attached through the nitrogen atom, compositions containing them, and their use for treating medical disorders where a decreased level of plasma free fatty acids (FFA) is desired.
Carbamate triserine lactone receptors for anion recognition
作者:Yizhe Wang、Edward Duran、David Nacionales、Amber Valencia、Christopher Wostenberg、Eric R. Marinez
DOI:10.1016/j.tetlet.2008.08.081
日期:2008.11
We have taken advantage of the ability of the cyclic triester of L-serine to organize ligand units appended to the three alpha-amine functionalities, as in enterobactin, a siderophore produced by enteric bacteria that binds ferric ion exceptionally well (K-f = 10(49)). As an extension of the preorganization concept, this work describes the preparation and characterization of carbamate triserine lactone receptors 1-6 and their ability to act as molecular receptors for anions. These receptors bind halides (F- >> Cl- > Br- > I-) with binding constants K in the range 21-7350 L mol(-1). (C) 2008 Elsevier Ltd. All rights reserved.
Carbazates as potent inhibitors of hormone-sensitive lipase
作者:Johannes C. de Jong、Lotte G. Sørensen、Hans Tornqvist、Poul Jacobsen
DOI:10.1016/j.bmcl.2004.01.038
日期:2004.4
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. (C) 2004 Elsevier Ltd. All rights reserved.