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The Discovery of acylated β-Amino acids as potent and orally bioavailable VLA-4 antagonists

Lin, Linus S ; Kopka, Ihor E ; Mumford, Richard A ; Magriotis, Plato A ; Lanza, Thomas ; Durette, Philippe L ; Kamenecka, Theodore ; Young, David N ; Laszlo, Stephen E.de ; Mccauley, Ermenegilda ; Riper, Gail Van ; Kidambi, Usha ; Egger, Linda A ; Tong, Xinchun ; Lyons, Kathryn ; Vincent, Stella ; Stearns, Ralph ; Colletti, Adria ; Teffera, Yohannes ; Fenyk-Melody, Judy ; Schmidt, John A ; Maccoss, Malcolm ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(4), pp.611-614 [Peer Reviewed Journal]

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Title:
The Discovery of acylated β-Amino acids as potent and orally bioavailable VLA-4 antagonists
Author: Lin, Linus S ; Kopka, Ihor E ; Mumford, Richard A ; Magriotis, Plato A ; Lanza, Thomas ; Durette, Philippe L ; Kamenecka, Theodore ; Young, David N ; Laszlo, Stephen E.de ; Mccauley, Ermenegilda ; Riper, Gail Van ; Kidambi, Usha ; Egger, Linda A ; Tong, Xinchun ; Lyons, Kathryn ; Vincent, Stella ; Stearns, Ralph ; Colletti, Adria ; Teffera, Yohannes ; Fenyk-Melody, Judy ; Schmidt, John A ; Maccoss, Malcolm ; Hagmann, William K
Description: Acylated β-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. Graphic
Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(4), pp.611-614
Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/S0960-894X(01)00818-6
Subjects: Medicine ; Chemistry ; Anatomy & Physiology
Language: English

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