922529-69-9Relevant academic research and scientific papers
4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist
Chiba, Jun,Iimura, Shin,Yoneda, Yoshiyuki,Sugimoto, Yuichi,Horiuchi, Takao,Muro, Fumito,Ochiai, Yuichi,Ogasawara, Tomomi,Tsubokawa, Masao,Iigou, Yutaka,Takayama, Gensuke,Taira, Tomoe,Takata, Yoshimi,Yokoyama, Mika,Takashi, Tohru,Nakayama, Atsushi,Machinaga, Nobuo
, p. 1515 - 1529 (2007/10/03)
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.
