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

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

Index: 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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Citation Number: 6

Abstract

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).