Article

Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.

Neurology Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW, UK.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 07/2008; 18(11):3392-9. DOI:10.1016/j.bmcl.2008.04.018 pp.3392-9
Source: PubMed

ABSTRACT Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated efficacy in the CFA model of inflammatory pain.

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Keywords

brain penetrant compounds
 
carboxylic acid group
 
CFA model
 
inflammatory pain
 

Adrian Hall