期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 24, 页码 7578-7583出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.10.042
关键词
Phosphoinositide 3-kinase gamma; 2-Amino-5-oxadiazolyl thiazole; The Ames test; Collagen induced arthritis (CIA) model
Class I phosphoinositide 3-kinases (PI3Ks), particularly PI3K gamma, have become attractive drug targets for inflammatory and autoimmune disorders such as rheumatoid arthritis. Herein, we describe the synthesis and the structure-activity relationships (SAR) of a series of 2-amino-5-oxadiazolyl thiazoles, culminating in the identification of 8j (TASP0415914), an orally potent inhibitor of phosphoinositide 3-kinase gamma (PI3K gamma). TASP0415914 demonstrated good potency in a cell-based assay and, furthermore, exhibited in vivo efficacy in a collagen induced arthritis (CIA) model in mice after oral administration. (C) 2013 Elsevier Ltd. All rights reserved.
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