4.5 Article

Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 15, 页码 4406-4409

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.062

关键词

CB2; Agonist; Lipophilicity; LiPE; Parallel synthesis

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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. (C) 2009 Elsevier Ltd. All rights reserved.

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