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Bioorg Med Chem Lett. 2009 Aug 1;19(15):4406-9. doi: 10.1016/j.bmcl.2009.05.062. Epub 2009 May 21.

Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis.

Author information

1
Pfizer Discovery Chemistry, Ramsgate Road, Sandwich CT139NJ Kent, United Kingdom. thomas.ryckmans@pfizer.com

Abstract

A series of libraries were designed using the 1-(cyclopropylmethyl)-2-alkyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-5-ium templates 2a-b, and Sulfonamide derivatives 11a-n proved to be potent agonists of the CB(2) receptor. Analysis of the Lipophilic Efficiency (LipE) of potent compounds provided new insight for the design of potent, metabolically stable CB2 agonists.

PMID:
19500981
DOI:
10.1016/j.bmcl.2009.05.062
[Indexed for MEDLINE]

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