Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu 4 positive allosteric modulators that mitigate CYP1A2 induction liability.

Darren W Engers,Sean R Bollinger,Julie L Engers,Joseph D Panarese,Megan M Breiner, Alison Gregro,Anna L Blobaum,Joanne J Bronson,Yong-Jin Wu,John E Macor,Alice L Rodriguez,Rocio Zamorano,P Jeffrey Conn,Craig W Lindsley,Colleen M Niswender,Corey R Hopkins

Bioorganic & Medicinal Chemistry Letters（2018）

引用 10|浏览22

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摘要

•A new indazole based mGlu4 PAM scaffold is reported.•This scaffold showed excellent potency, selectivity and brain penetration.•A detailed SAR analysis around the CYP induction issue that has plagued previous scaffolds.

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关键词

mGlu4 PAM,Positive allosteric modulator,CYP induction,Parkinson’s disease,Structure-activity relationship

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