774607-79-3Relevant academic research and scientific papers
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists
Cramp, Sue,Dyke, Hazel J.,Higgs, Christopher,Clark, David E.,Gill, Matthew,Savy, Pascal,Jennings, Neil,Price, Steve,Lockey, Peter M.,Norman, Dennis,Porres, Soraya,Wilson, Francis,Jones, Alison,Ramsden, Nigel,Mangano, Raffaella,Leggate, Dan,Andersson, Marie,Hale, Richard
scheme or table, p. 2516 - 2519 (2010/06/20)
The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H4 receptor inverse agonists is described. The initial hit, 3A (IC50 19 nM) was identified by means of a ligand-based virtual screening approach. Subsequent medicinal chemistry exploration yielded 18I which possessed increased potency (R-enantiomer IC50 1 nM) as well as enhanced microsomal stability.
AMINO PYRIMIDINE COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
-
Page/Page column 24-25, (2010/11/28)
The present invention relates to novel amino pyrimidine compounds of formula (I) for the modulation of the histamine H4 receptor and the treatment or prevention of conditions mediated by the histamine H4 receptor. The invention also relates to the preparation of such compounds.
Pyrimidines and uses thereof
-
, (2008/06/13)
The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells.
Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: Inhibitors of lysophosphatidic acid acyltransferase-β
Gong, Baoqing,Hong, Feng,Kohm, Cory,Jenkins, Scott,Tulinsky, John,Bhatt, Rama,De Vries, Peter,Singer, Jack W.,Klein, Peter
, p. 2303 - 2308 (2007/10/03)
2,4-Diamino-N4,6-diarylpyrimidines were identified as potent, isoform specific inhibitors of lysophosphatidic acid acyltransferase-β (LPAAT-β). Active inhibitors also blocked proliferation of tumor cell lines in vitro. The effect of 2j in an in
