Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Leifeng Cheng"'
Autor:
Robert J. Sheppard, Peter Schell, Eelke B. Lenselink, Leifeng Cheng, Laura H. Heitman, Adriaan P. IJzerman, Henk de Vries, Maria J. Petersson, Roine I. Olsson, Sara Pahlén, Michael J. Waring, Lizi Xia, Julien Louvel
Publikováno v:
Journal of Medicinal Chemistry
JOURNAL OF MEDICINAL CHEMISTRY, 60(23), 9545-9564
JOURNAL OF MEDICINAL CHEMISTRY
JOURNAL OF MEDICINAL CHEMISTRY, 60(23), 9545-9564
JOURNAL OF MEDICINAL CHEMISTRY
We report on the synthesis and biological evaluation of a series of 1,2-diarylimidazol-4-carboxamide derivatives developed as CB1 receptor antagonists. These were evaluated in a radioligand displacement binding assay, a [35S]GTPγS binding assay, and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff212f527a82b848d9f47dfc77c4462a
https://hdl.handle.net/1887/58213
https://hdl.handle.net/1887/58213
Autor:
Göran Wahlund, Yafeng Xue, Jonas Boström, Alleyn T. Plowright, Bengt Ohlsson, Leifeng Cheng, Sara Pahlén, Tomas Fex, Lars-Olof Larsson, Daniel Pettersen, Walter Lindberg, Maria Jonforsen, Emma Evertsson, Anders Thelin, David Gustafsson, Michael Karle, Constanze Hilgendorf, Peter Schell
Publikováno v:
ACS Medicinal Chemistry Letters. 5:538-543
A class of novel oral fibrinolysis inhibitors has been discovered, which are lysine mimetics containing an isoxazolone as a carboxylic acid isostere. As evidenced by X-ray crystallography the inhibitors bind to the lysine binding site in plasmin thus
Autor:
Leifeng Cheng, Georges Vauquelin, John C. Clapham, Marie Wennerberg, Stephan Hjorth, Anudharan Balendran
Publikováno v:
Fundamental & Clinical Pharmacology. 25:200-210
The implication of the cannabinoid receptor 1 (CB(1) receptor) in several pathophysiological states has sparked the development of selective antagonists. Here we compare binding of the antagonists [(3) H]-AZ12491187, [(3) H]-taranabant and [(3) H]-ri
Publikováno v:
Synthetic Communications. 37:2793-2806
The regioselective syntheses of two pharmaceutically relevant pyrrole scaffolds are described. A synthetic route for the preparation of differentially substituted pyrrole‐3,4‐dicarboxylates is presented and exemplified. This route circumvents som
Autor:
Lizi Xia, de Vries, Henk, Lenselink, Eelke B., Louvel, Julien, Waring, Michael J., Leifeng Cheng, Pahlén, Sara, Petersson, Maria J., Schell, Peter, Olsson, Roine I., Heitman, Laura H., Sheppard, Robert J., IJzerman, Adriaan P.
Publikováno v:
Journal of Medicinal Chemistry; 12/14/2017, Vol. 60 Issue 23, p9545-9564, 20p
Autor:
Marie, Wennerberg, Leifeng, Cheng, Stephan, Hjorth, John C, Clapham, Anudharan, Balendran, Georges, Vauquelin
Publikováno v:
Fundamentalclinical pharmacology. 25(2)
The implication of the cannabinoid receptor 1 (CB(1) receptor) in several pathophysiological states has sparked the development of selective antagonists. Here we compare binding of the antagonists [(3) H]-AZ12491187, [(3) H]-taranabant and [(3) H]-ri
Publikováno v:
Journal of Medicinal Chemistry. 35:3364-3369
Ketomethylene pseudopeptide analogues Aa-Pro-Arg psi (COCH2) Gly-pip, 1, where Aa are D- or L-amino acids (Dpa, beta, beta-diphenylalanine; alpha Nal, alpha-naphthylalanine; beta Nal, beta-naphthylalanine; Fgl, fluorenylglycine) with highly lipophili
Autor:
Erik Ryberg, Leifeng Cheng, Henrik Nordberg, Jonas Boström, Roine I. Olsson, Peter J. Greasley, Joakim Tholander, Stephan Hjorth
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(2)
A novel class of cannabinoid-1 (CB1) receptor antagonists for the treatment of obesity is presented. The carboxamide linker in a set of 5,6-diaryl-pyrazine-2-amide derivatives was transformed into the corresponding thioamide, by using a one-pot synth
Publikováno v:
Tetrahedron Letters. 32:7333-7336
Novel phosphorus-containing peptidomimetics, D-Aa-Pro-Aa P (OPh) 2 , with lipophilic amino acids at the P 3 positions 1 and amino phosphonic acids with neutral side chains in the P 1 position have been designed and synthesized as thrombin inhibitors.
Autor:
Hermann Robert Bell, Ann M. McNulty, Stephen L. Cooper, Gerald W. Becker, Robert M. Adlington, Beining Chen, Leifeng Cheng, Trevor J. Howe, William McCoull, Jack E. Baldwin, Blake Lee Neubauer, Gareth J. Pritchard
Publikováno v:
Journal of medicinal chemistry. 44(10)
A homology derived molecular model of prostate specific antigen (PSA) was created and refined. The active site region was investigated for specific interacting functionality and a binding model postulated for the novel 2-azetidinone acyl enzyme inhib