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  • Title: The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
    Author: Lin LS, Kopka IE, Mumford RA, Magriotis PA, Lanza T, Durette PL, Kamenecka T, Young DN, de Laszlo SE, McCauley E, Riper GV, Kidambi U, Egger LA, Tong X, Lyons K, Vincent S, Stearns R, Colletti A, Teffera Y, Fenyk-Melody J, Schmidt JA, MacCoss M, Hagmann WK.
    Journal: Bioorg Med Chem Lett; 2002 Feb 25; 12(4):611-4. PubMed ID: 11844683.
    Abstract:
    Acylated beta-amino acids are described as potent, specific and orally bioavailable antagonists of VLA-4. The initial lead was identified from a combinatorial library. Subsequent optimization using a traditional medicinal chemistry approach led to significant improvement in potency (up to 8-fold) while maintaining good pharmacokinetic properties.
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