Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis |
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| Authors: | Thomas Ryckmans Martin P. Edwards Val A. Horne Ana Monica Correia Dafydd R. Owen Lisa R. Thompson Isabelle Tran Michelle F. Tutt Tim Young |
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| Affiliation: | 1. Pfizer Discovery Chemistry, Ramsgate Road, Sandwich CT139NJ Kent, United Kingdom;2. Pfizer Global Research and Development, La Jolla Laboratories, 10770 Science Center Drive, San Diego, CA 92121, USA;3. Pfizer Discovery Biology, Ramsgate Road, Sandwich CT139NJ Kent, United Kingdom |
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| 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. |
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