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. 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

Thomas Ryckmans  1 , Martin P Edwards, Val A Horne, Ana Monica Correia, Dafydd R Owen, Lisa R Thompson, Isabelle Tran, Michelle F Tutt, Tim Young
Affiliations

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

Thomas Ryckmans et al. Bioorg Med Chem Lett. .

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.

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