1245816-48-1Relevant articles and documents
Synthesis and biological activity of a series of tetrasubstituted- imidazoles as P2X7 antagonists
Gleave, Robert J.,Walter, Daryl S.,Beswick, Paul J.,Fonfria, Elena,Michel, Anton D.,Roman, Shilina A.,Tang, Sac-Pham
scheme or table, p. 4951 - 4954 (2010/10/04)
A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity relationships (SAR) were investigated both with respect to activity at the P2X7 receptor and in vitro metabolic stability. Compound 10 was identified as a potent P2X7 antagonist with reduced in vitro metabolism and high solubility.