499120-83-1Relevant articles and documents
Improving metabolic stability of phosphodiesterase-4 inhibitors containing a substituted catechol: Prevention of reactive intermediate formation and covalent binding
Chauret, Nathalie,Guay, Daniel,Li, Chun,Day, Stephen,Silva, José,Blouin, Marc,Ducharme, Yves,Yergey, James A.,Nicoll-Griffith, Deborah A.
, p. 2149 - 2152 (2007/10/03)
A detailed study directed towards metabolic stability optimization of the alkoxy substituents on the catechol moiety of CDP-840 is reported. Replacement of the methoxy and cyclopentyloxy substituents by cyclobutyloxy and/or difluromethoxy groups resulted in the discovery of potent and selective PDE4 inhibitors where the formation of reactive metabolites that could covalently bind to microsomal protein was significantly reduced or eliminated.