Identification of a sulfonamide series of CCR2 antagonists

被引：24
|
作者：
Peace, Simon [1 ]
Philp, Joanne [2 ]
Brooks, Carl [2 ]
Piercy, Val [1 ]
Moores, Kitty [1 ]
Smethurst, Chris [3 ]
Watson, Steve [3 ]
Gaines, Simon [1 ]
Zippoli, Mara [1 ]
Mookherjee, Claudette [3 ]
Ife, Robert [1 ]
机构：
[1] GlaxoSmithKline Med Res Ctr, Stevenage SG1 2NY, Herts, England
[2] GlaxoSmithKline, Upper Mer, King Of Prussia, PA 19406 USA
[3] GlaxoSmithKline, Harlow CM19 5MW, Essex, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 13期
关键词：
CCR2; antagonists; pK(a); Sulfonamides; SMALL-MOLECULE; POTENT; CHEMOKINES; EXPRESSION;
D O I：
10.1016/j.bmcl.2010.04.142
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3961 / 3964
页数：4
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