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Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors

…, KT Symons, PM Nguyen, ME Massari, S Dozier…

文献索引:Gahman, Timothy C.; Herbert, Mark R.; Lang, Henk; Thayer, Angie; Symons, Kent T.; Nguyen, Phan Manh; Massari, Mark E.; Dozier, Sara; Zhang, Yan; Sablad, Marciano; Rao, Tadimeti S.; Noble, Stewart A.; Shiau, Andrew K.; Hassig, Christian A. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 22 p. 6888 - 6894

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被引用次数: 6

摘要

We have identified and synthesized a series of imidazole containing dimerization inhibitors of inducible nitric oxide synthase (iNOS). The necessity of key imidazole and piperonyl functionality was demonstrated and SAR studies led to the identification of compound 35, which showed a dose dependant inhibition in multiple pain models, including tactile allodynia induced by spinal nerve ligation (Chung model).