273939-47-2Relevant articles and documents
Design of novel and potent cPLA2α inhibitors containing an α-methyl-2-ketothiazole as a metabolically stable serine trap
Mete, Antonio,Andrews, Glen,Bernstein, Mike,Connolly, Stephen,Hartopp, Paul,Jackson, Clive G.,Lewis, Richard,Martin, Iain,Murray, David,Riley, Rob,Robinson, David H.,Smith, Gill M.,Wells, Edward,Withnall, W. John
scheme or table, p. 3128 - 3133 (2011/06/24)
We report the design of novel, potent cPLA2α inhibitors that possess an α-methyl-2-ketothiazole that acts as a serine-reactive moiety. We describe the optimization of the series for potency and metabolic stability towards ketone reduction. This