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  • Title: Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.
    Author: Chiba J, Machinaga N, Takashi T, Ejima A, Takayama G, Yokoyama M, Nakayama A, Baldwin JJ, McDonald E, Moriarty KJ, Sarko CR, Saionz KW, Swanson R, Hussain Z, Wong A.
    Journal: Bioorg Med Chem Lett; 2005 Jan 03; 15(1):41-5. PubMed ID: 15582407.
    Abstract:
    An investigation into the structure-activity relationship of a lead compound, prolyl-5-aminopentanoic acid 4, led to the identification of a novel series of 4-piperidinylacetic acid, 1-piperazinylacetic acid, and 4-aminobenzoic acid derivatives as potent VLA-4 antagonists with low nanomolar IC(50) values. A representative compound morpholinyl-4-piperidinylacetic acid derivative (13d: IC(50)=4.4 nM) showed efficacy in the Ascaris-antigen sensitized murine airway inflammation model by oral administration.
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