Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X7 antagonists
| Autor: | Sac-Pham Tang, Robert Gleave, Paul John Beswick, Anton D. Michel, Shilina Roman, Daryl S. Walter, Elena Fonfria |
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| Rok vydání: | 2010 |
| Předmět: |
medicine.drug_class
Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Pyrazole Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Purinergic P2 Receptor Antagonists medicine Animals Humans Structure–activity relationship Imidazole Molecular Biology Receptors Purinergic P2 Anti-Inflammatory Agents Non-Steroidal Organic Chemistry Imidazoles Antagonist Biological activity In vitro Rats chemistry Pyrazoles Molecular Medicine Receptors Purinergic P2X7 |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:4951-4954 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.05.018 |
| Popis: | 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 P2X(7) receptor and in vitro metabolic stability. Compound 10 was identified as a potent P2X(7) antagonist with reduced in vitro metabolism and high solubility. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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