Guo-Hua Chu, Bertrand Le Bourdonnec, Minghua Gu, Christopher W Ajello, Lara K Leister, Ian Sellitto, Joel A Cassel, Paul A Tuthill, Heather O' Hare, Robert N Dehaven, Roland E Dolle
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引用次数: 0
摘要
我们合成了一系列通式为 I 的咪唑嘧啶衍生物,并确定它们是 iNOS 二聚体形成的强效抑制剂,而 iNOS 二聚体的形成是该酶正常工作的前提条件。Stille 和 Negishi 偶联反应是形成连接咪唑嘧啶核心与中央环烯基、环烷基和苯基环模板的碳-碳键的关键步骤。
Design and Synthesis of Imidazopyrimidine Derivatives as Potent iNOS Dimerization Inhibitors.
A series of imidazopyrimidine derivatives with the general formula I was synthesized and identified as potent inhibitors of iNOS dimer formation, a prerequisite for proper functioning of the enzyme. Stille and Negishi coupling reactions were used as key steps to form the carbon-carbon bond connecting the imidazopyrimidine core to the central cycloalkenyl, cycloalkyl and phenyl ring templates.