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Resolving Inflammation: Synthesis, Configurational Assignment, and Biological Evaluations of RvD1.
Tungen, Jørn Eivind Gerstmann, Lisa Vik, Anders De Matteis, Roberta Colas, Romain Alexandre Dalli, Jesmond Chiang, Nan Serhan, Charles Nicholas Hansen, Trond Vidar
Tungen, Jørn Eivind
Gerstmann, Lisa
Vik, Anders
De Matteis, Roberta
Colas, Romain Alexandre
Dalli, Jesmond
Chiang, Nan
Serhan, Charles Nicholas
Hansen, Trond Vidar
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2018-12-20
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Abstract
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 RvD1n-3 DPA has been achieved using the underutilized sp3 -sp3 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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Chemistry. 2019 Jan 28;25(6):1476-1480. doi: 10.1002/chem.201806029. Epub 2018 Dec 20.
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en
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1521-3765