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  • Title: 4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist.
    Author: Chiba J, Iimura S, Yoneda Y, Sugimoto Y, Horiuchi T, Muro F, Ochiai Y, Ogasawara T, Tsubokawa M, Iigou Y, Takayama G, Taira T, Takata Y, Yokoyama M, Takashi T, Nakayama A, Machinaga N.
    Journal: Chem Pharm Bull (Tokyo); 2006 Nov; 54(11):1515-29. PubMed ID: 17077548.
    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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