Discovery of Novel 2-Anilinopyrazolo[1,5-a]pyrimidine Derivatives as c-Src Kinase Inhibitors for the Treatment of Acute Ischemic Stroke

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概要

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• 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.

• 公益社団法人日本薬学会の論文
• 2007-06-01

著者

• Kusama Hiroshi

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Kusama Hiroshi

  Central Research Laboratories Kissei Pharmaceutical Co. Ltd.

• NISHIMURA Toshihiro

  Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.

• Kamada Noboru

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Kikuchi Shinji

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• MUKAIYAMA Harunobu

  Central Research Laboratory, Kissei Pharmaceutical Company Ltd.

• SHIOHARA Hiroaki

  Central Research Laboratory, Kissei Pharmaceutical Company Ltd.

• KOBAYASHI Satoko

  Central Research Laboratory, Kissei Pharmaceutical Company Ltd.

• KOMATSU Yoshimitsu

  Central Research Laboratory, Kissei Pharmaceutical Company Ltd.

• TSUJI Eiichi

  Central Research Laboratory, Kissei Pharmaceutical Company Ltd.

• OHNOTA Hideki

  Central Research Laboratory, Kissei Pharmaceutical Company Ltd.

• Shiohara Hiroaki

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Tsuji Eiichi

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Ohnota Hideki

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Ohnota Hideki

  Central Research Laboratories Kissei Pharmaceutical Co. Ltd.

• Kobayashi Satoko

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Mukaiyama Harunobu

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Komatsu Yoshimitsu

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

• Nishimura Toshihiro

  Central Research Laboratory Kissei Pharmaceutical Company Ltd.

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