Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases

Class I phosphoinositide 3-kinases (PI3Ks), particularly PI3Kγ, 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,...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2013-12, Vol.21 (24), p.7578-7583
Hauptverfasser:	Oka, Yusuke, Yabuuchi, Tetsuya, Oi, Takahiro, Kuroda, Shoichi, Fujii, Yasuyuki, Ohtake, Hidenori, Inoue, Tomoyuki, Wakahara, Shunichi, Kimura, Kayo, Fujita, Kiyoko, Endo, Mayumi, Taguchi, Kyoko, Sekiguchi, Yoshinori
Format:	Artikel
Sprache:	eng
Schlagworte:	2-Amino-5-oxadiazolyl thiazole Administration, Oral Animals Arthritis, Experimental - chemically induced Arthritis, Experimental - drug therapy Arthritis, Experimental - enzymology Class Ib Phosphatidylinositol 3-Kinase - antagonists & inhibitors Class Ib Phosphatidylinositol 3-Kinase - metabolism Collagen Collagen induced arthritis (CIA) model Disease Models, Animal Dose-Response Relationship, Drug Drug Discovery drugs Enzyme Inhibitors - administration & dosage Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Male Mice Mice, Inbred DBA Molecular Structure oral administration Oxadiazoles - administration & dosage Oxadiazoles - chemistry Oxadiazoles - pharmacology phosphatidylinositol 3-kinase Phosphoinositide 3-kinase γ rheumatoid arthritis Structure-Activity Relationship structure-activity relationships The Ames test thiazoles Thiazoles - administration & dosage Thiazoles - chemistry Thiazoles - pharmacology
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