Re-exploration of the mGlu(1) PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR

This letter describes the re-exploration of the mGlu(1) PAM Ro 07-11401 scaffold through a multi-dimensional, iterative parallel synthesis approach. Unlike recent series of mGlu(1) PAMs with robust SAR, the SAR around the Ro 07-11401 structure was incredibly steep (only ~6 of 200 analogs displayed m...

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Veröffentlicht in:Bioorg Med Chem Lett
Hauptverfasser: Garcia-Barrantes, Pedro M., Cho, Hyekyung P., Starr, Tahj M., Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2016
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4833523/
https://ncbi.nlm.nih.gov/pubmed/27013388
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.03.044
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