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

被引：238

作者：

Ryckmans, Thomas ^{[1
]}

Edwards, Martin P. ^{[2
]}

Horne, Val A. ^{[1
]}

Correia, Ana Monica ^{[3
]}

Owen, Dafydd R. ^{[1
]}

Thompson, Lisa R. ^{[1
]}

Tran, Isabelle ^{[1
]}

Tutt, Michelle F. ^{[3
]}

Young, Tim ^{[3
]}

机构：

[1] Pfizer Discovery Chem, Sandwich CT13 9NJ, Kent, England

[2] Pfizer Global Res & Dev, La Jolla Labs, San Diego, CA 92121 USA

[3] Pfizer Discovery Biol, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 15期

关键词：

CB2; Agonist; Lipophilicity; LiPE; Parallel synthesis; RECEPTOR;

D O I：

10.1016/j.bmcl.2009.05.062

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：4406 / 4409

页数：4

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