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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6144-7. doi: 10.1016/j.bmcl.2009.09.016. Epub 2009 Sep 11.

Optimising metabolic stability in lipophilic chemical space: the identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonist.

Author information

1
Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. duncan.miller@pfizer.com

Abstract

Balancing potency and metabolic stability in a target which favours lipophilic ligands is a considerable challenge. Here we describe two strategies employed to achieve this balance in a series of pyrazolopyrimidine CRF antagonists: moderation of lipophilicity, and incorporation of a metabolically stable lipophilic group.

PMID:
19782566
DOI:
10.1016/j.bmcl.2009.09.016
[Indexed for MEDLINE]

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