Department of Medicinal Chemistry, Kalypsys Inc., 10420 Wateridge Circle, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6888-94. doi: 10.1016/j.bmcl.2011.08.112. Epub 2011 Sep 8.
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).
我们已经鉴定并合成了一系列诱导型一氧化氮合酶(iNOS)的二聚抑制剂。关键咪唑和哌啶基功能的必要性已经得到证明,SAR 研究导致了化合物 35 的鉴定,该化合物在多种疼痛模型中表现出剂量依赖性抑制作用,包括脊神经结扎引起的触觉过敏(Chung 模型)。