Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase γ inhibitors

被引：27
|
作者：
Oka, Yusuke [1 ]
Yabuuchi, Tetsuya [1 ]
Fujii, Yasuyuki [2 ]
Ohtake, Hidenori [2 ]
Wakahara, Shunichi [2 ]
Matsumoto, Kayo [2 ]
Endo, Mayumi [1 ]
Tamura, Yunoshin [1 ]
Sekiguchi, Yoshinori [1 ]
机构：
[1] Taisho Pharmaceut Co Ltd, Med Chem Labs, Kita Ku, Saitama 3319530, Japan
[2] Taisho Pharmaceut Co Ltd, Mol Funct & Pharmacol Labs, Kita Ku, Saitama 3319530, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 24期
关键词：
Phosphoinositide; 3-kinase; PI3K gamma inhibitor; 2-Aminothiazole-oxazoles; PI3K-GAMMA; INFLAMMATION;
D O I：
10.1016/j.bmcl.2012.10.028
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of 2-aminothiazole-oxazoles was designed and synthesized as part of efforts to develop potent phosphoinositide 3-kinase gamma (PI3K gamma) inhibitors. The modification of a high-throughput screening hit, compound 1, resulted in the identification of compounds 10 and 15, which displayed potent inhibitory activities in enzyme-based and cell-based assays. (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码：7534 / 7538
页数：5
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