Rapid assessment of a novel series of selective CB 2 agonists using parallel synthesis protocols: a lipophilic efficiency (LipE) analysis

…, MP Edwards, VA Horne, AM Correia, DR Owen…

Index: Ryckmans, Thomas; Edwards, Martin P.; Horne, Val A.; Correia, Ana Monica; Owen, Dafydd R.; Thompson, Lisa R.; Tran, Isabelle; Tutt, Michelle F.; Young, Tim Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4406 - 4409

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Citation Number: 137

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 CB2 receptor. Analysis of the Lipophilic Efficiency (LipE) of potent compounds provided new insight for the design of potent, metabolically stable CB2 agonists.