Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Discovery of Novel 2-Anilinopyrazolo[1,5-a]pyrimidine Derivatives as c-Src Kinase Inhibitors for the Treatment of Acute Ischemic Stroke
Harunobu Mukaiyama, Toshihiro Nishimura, Hiroaki Shiohara, Satoko Kobayashi, Yoshimitsu Komatsu, Shinji Kikuchi, Eiichi Tsuji, Noboru Kamada, Hideki Ohnota, Hiroshi Kusama
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Keywords: c-Src kinase, pyrazolo[1,5-a]pyrimidine, acute ischemic stroke, central nervous system penetration
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2007 Volume 55 Issue 6 Pages 881-889

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Abstract

We synthesized a series of novel 2-anilinopyrazolo[1,5-a]pyrimidine derivatives and evaluated their ability to inhibit c-Src kinase; 7-(2-amino-2-methylpropylamino)-5-cyclopropyl-2-(3,5-dimethoxyphenylamino)pyrazolo[1,5-a]pyrimidine-3-carboxamide 7o and 7-(2-amino-2-methylpropylamino)-2-(3,5-dimethoxyphenylamino)-5-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide 7f showed potent inhibitory activity. Compound 7f inhibited c-Src selectively and exhibited satisfactory central nervous system (CNS) penetration. Furthermore, 7f·HCl reduced the infarct volume in vivo in a rat middle cerebral artery (MCA) occlusion model when administrated intraperitoneally.

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© 2007 The Pharmaceutical Society of Japan
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