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Bioorg Med Chem Lett. 2012 Feb 1;22(3):1335-9. doi: 10.1016/j.bmcl.2011.12.080. Epub 2011 Dec 21.

Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound.

Author information

1
Department of Chemical Research-CV & CNS, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. william.mcelroy@merck.com

Abstract

A series of pyrazoloquinolines, possessing (hetero)arylhydroxymethyl substituents at the quinoline C-4 position were evaluated as PDE10A inhibitors. Among these, methylpyrimidyl analogue 15 was identified as having good rodent and monkey exposure, and a MED of 10 mg/kg in an in vivo model.

PMID:
22227212
DOI:
10.1016/j.bmcl.2011.12.080
[Indexed for MEDLINE]

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