4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist.

  title={4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist.},
  author={Jun Chiba and Shin Iimura and Yoshiyuki Yoneda and Yuichi Sugimoto and Takao Horiuchi and Fumito Muro and Yuichi Ochiai and Tomomi Ogasawara and Masao Tsubokawa and Yutaka Iigou and Gensuke Takayama and Tomoe Taira and Yoshimi Takata and Mika Yokoyama and Tohru Takashi and Atsushi Nakayama and Nobuo Machinaga},
  journal={Chemical & pharmaceutical bulletin},
  volume={54 11},
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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Annual Report in Medicinal Chemistry,

G W.Holland, R J.Biediger, P. Vandersilice

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