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Discovery of novel central nervous system penetrant metabotropic glutamate receptor subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) based o…

A new interesting article has been published in J Med Chem. 2018 Oct 23. doi: 10.1021/acs.jmedchem.8b01266. [Epub ahead of print] and titled:

Discovery of novel central nervous system penetrant metabotropic glutamate receptor subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) based o…

Authors of this article are:

Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW.

A summary of the article is shown below:

A scaffold hopping exercise from a monocyclic mGlu2 NAM with poor rodent PK led to two novel heterobicyclic series of mGlu2 NAMs based on either a functionalized pyrazolo[1,5-a]pyrimidine-5-carboxamide core or a thieno[3,2-b]pyridine-5-carboxamide core. These novel analogs secured an intellectual property position and possessed enhanced rodent PK, while also maintaining good mGlu2 NAM potency, selectivity (versus mGlu3 and the remaining six mGlu receptors) and high CNS penetration. Interestingly, SAR was divergent between the new 5,6-heterobicyclic systems.

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