Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.

Scott D Kuduk,Jason W Skudlarek,Christina N Di Marco,Joseph G Bruno,Mark A Pausch,Julie A O'Brien,Tamara D Cabalu,Joanne Stevens,Joseph Brunner,Pamela L Tannenbaum,Anthony L Gotter,Christopher J Winrow,John J Renger,Paul J Coleman

Bioorganic & Medicinal Chemistry Letters（2014）

引用 16|浏览12

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摘要

Replacement of the ether linkage in the filorexant proved highly sensitive toward modification with an acetylene linkage providing compounds with the best in vitro and in vivo potency profiles.

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关键词

Orexin,Insomnia,Antagonist

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