Structure-Activity Relationships of 2-(Benzothiazolylthio)acetamide Class of CCR3 Selective Antagonist

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概要

• 論文の詳細を見る

• The structure activity relationships of novel selective CCR3 receptor antagonists, 2-(benzothiazolylthio)acetamimde derivatives were described. A lead structure (1a) was discovered from the screening of the focused library that was based on the structure of our dual antagonists for the human CCR1 and CCR3 receptors. Derivatization of la including incorporation of substituent(s) into each benzene ring of the benzothiazole and piperidine side chain resulted in the identification of potent and selective compounds (1b,r,s) exhibiting nano-molar binding affinity (IC_<50>s: 1.5-3.0nM) and greater than 800-fold selectivity for the CCR3 receptor over the CCR1 receptor.

• 公益社団法人日本薬学会の論文
• 2003-06-01

著者

• Ohwaki Kenji

  Banyu Pharmaceutical Co,. Ltd

• Kobayashi K

  Banyu Tsukuba Research Institute

• Ishikawa M

  Banyu Tsukuba Research Institute

• NAYA Akira

  Banyu Tsukuba Research Institute

• KOBAYASHI Kensuke

  Banyu Tsukuba Research Institute

• ISHIKAWA Makoto

  Banyu Tsukuba Research Institute

• SAEKI Toshihiko

  Banyu Tsukuba Research Institute

• NOGUCHI Kazuhito

  Banyu Tsukuba Research Institute

• OHTAKE Norikazu

  Banyu Tsukuba Research Institute

• Saeki T

  Banyu Tsukuba Research Institute

• Ohtake N

  Banyu Tsukuba Research Institute

• Noguchi K

  Banyu Tsukuba Research Institute

• Ohwaki K

  Banyu Tsukuba Research Institute

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• Structure-Activity Relationships of 2-(Benzothiazolylthio)acetamide Class of CCR3 Selective Antagonist
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