Resolving Inflammation: Synthesis, Configurational Assignment, and Biological Evaluations of RvD1(n-3 DPA)
Chemistry(2018)
摘要
New drugs that can resolve inflammation without immunosuppressive effects are at the medicinal chemistry frontier. Pro-resolving endogenously formed small molecules, that is, the resolvins, are excellent candidates displaying such bioactions. The first total synthesis of the specialized pro-resolving mediator RvD1(n-3 DPA) has been achieved using the underutilized sp(3)-sp(3) Negishi cross coupling reaction and an alkyne hydrosilylation-protodesilylation protocol. Biological evaluations revealed that this novel mediator displays low nanomolar pro-resolving properties and potently activates the human DRV1/GPR32 receptor. As such, this endogenous natural product is a lead compound for the development of novel immunoresolvents.
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关键词
Karstedt's catalyst,natural products,sp(3)-sp(3) cross-coupling,specialized pro-resolving mediators,total synthesis
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