27412-77-7Relevant academic research and scientific papers
Identification of novel pyrazole acid antagonists for the EP1 receptor
McKeown, Stephen C.,Hall, Adrian,Giblin, Gerard M.P.,Lorthioir, Olivier,Blunt, Richard,Lewell, Xiao Q.,Wilson, Richard J.,Brown, Susan H.,Chowdhury, Anita,Coleman, Tanya,Watson, Stephen P.,Chessell, Iain P.,Pipe, Adrian,Clayton, Nick,Goldsmith, Paul
, p. 4767 - 4771 (2007/10/03)
The discovery, synthesis and structure-activity relationship (SAR) of a novel series of EP1 receptor antagonists is described. Pyrazole acid 4, identified from a chemical array, had desirable physicochemical properties, an excellent in vitro microsomal inhibition and cytochrome P450 (CYP450) profile and good exposure levels in blood. This compound had an ED50 of 1.3 mg/kg in a rat pain model. A range of more potent analogues in the in vitro assay was identified using efficient array chemistry. These EP1 antagonists have potential as agents in the treatment of PGE2 mediated pain.
Hydrazide-containing inhibitors of HIV-1 integrase
Zhao, He,Neamati, Nouri,Sunder, Sanjay,Hong, Huixiao,Wang, Shaomeng,Milne, George W. A.,Pommier, Yves,Burke Jr., Terrence R.
, p. 937 - 941 (2007/10/03)
Inhibitors of HIV integrase are currently being sought as potential new therapeutics for the treatment of AIDS. A large number of inhibitors discovered to date contain the o-bis-hydroxy catechol structure. In an effort to discover structural leads for the
