| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371388 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert J. Gleave, Daryl S. Walter, Paul J. Beswick, Elena Fonfria, Anton D. Michel, Shilina A. Roman, Sac-Pham Tang,