Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI

[Image: see text] Investigation of a novel amino-aza-benzimidazolone structural class of positive allosteric modulators (PAMs) of metabotropic glutamate receptor 2 (mGluR2) identified [2.2.2]-bicyclic amine 12 as an intriguing lead structure due to its promising physicochemical properties and lipoph...

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Vydáno v:ACS Med Chem Lett
Hlavní autoři: Pero, Joseph E., Rossi, Michael A., Kelly, Michael J., Lehman, Hannah D. G. F., Layton, Mark E., Garbaccio, Robert M., O’Brien, Julie A., Magliaro, Brian C., Uslaner, Jason M., Huszar, Sarah L., Fillgrove, Kerry L., Tang, Cuyue, Kuo, Yuhsin, Joyce, Leo A., Sherer, Edward C., Jacobson, Marlene A.
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2016
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4789683/
https://ncbi.nlm.nih.gov/pubmed/26985321
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00459
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