Surveying heterocycles as amide bioisosteres within a series of mGlu 7 NAMs: Discovery of VU6019278.

Carson W Reed,Jordan P Washecheck, Marc C Quitlag,Matthew T Jenkins,Alice L Rodriguez,Darren W Engers,Anna L Blobaum,P Jeffrey Conn,Colleen M Niswender,Craig W Lindsley

Bioorganic & Medicinal Chemistry Letters（2019）

引用 13|浏览25

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摘要

•Novel series of selective and CNS penetrant mGlu7 NAMs.•Identified a 1,3,4-oxadiazole as biosiostere for a labile amide linker.•Iterative libraries quickly optimized this novel tricyclic series.

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关键词

mGlu7,Metabotropic glutamate receptor,Negative allosteric modulator (NAM),Structure-activity relationship (SAR),VU6019278

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