Identification of trans-4-[1-[[7-fluoro-2-(1-methyl-3-indolyl)-6-benzoxazolyl]acetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid as a potent, orally active VLA-4 antagonist.

Masaki Setoguchi,Shin Iimura,Yuuichi Sugimoto,Yoshiyuki Yoneda,Jun Chiba,Toshiyuki Watanabe,Fumihito Muro,Yutaka Iigo,Gensuke Takayama,Mika Yokoyama,Tomoe Taira,Misato Aonuma,Tohru Takashi,Atsushi Nakayama,Nobuo Machinaga

Bioorganic & Medicinal Chemistry（2012）

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摘要

Compound 7e with 7-fluoro-2-(1-methyl-1H-indol-3-yl)-1,3-benzoxazolyl group significantly inhibited eosinophil infiltration into bronchoalveolar lavage fluid at 15mg/kg in an Ascaris-antigen-induced murine bronchial inflammatory model.

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关键词

VLA-4,Integrin,Eosinophil infiltration,Asthma

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