Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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4-(Pyrrolidinyl)methoxybenzoic Acid Derivatives as a Potent, Orally Active VLA-4 Antagonist
Jun Chiba, Shin Iimura, Yoshiyuki Yoneda, Yuichi Sugimoto, Takao Horiuchi, Fumito Muro, Yuichi Ochiai, Tomomi Ogasawara, Masao Tsubokawa, Yutaka Iigou, Gensuke Takayama, Tomoe Taira, Yoshimi Takata, Mika Yokoyama, Tohru Takashi, Atsushi Nakayama, Nobuo Machinaga
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Keywords: VLA-4, integrin, human serum albumin, asthma
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2006 Volume 54 Issue 11 Pages 1515-1529

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Abstract

A novel series of benzoic acid derivatives as VLA-4 antagonists were synthesized. Optimization, focusing on activity and lipophilicity needed for cell permeability, resulted in the identification of 15b and 15e with good activity (IC50=1.6 nM each) and moderate lipophilicity (Log D=2.0, 1.8). Furthermore, 15e demonstrated efficacy in murine asthma model by an oral dose of 30 mg/kg.

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© 2006 The Pharmaceutical Society of Japan
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