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Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists |
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| Authors: | Kopka Ihor E Lin Linus S Mumford Richard A Lanza Thomas Magriotis Plato A Young David DeLaszlo Stephen E MacCoss Malcolm Mills Sander G Van Riper Gail McCauley Ermengilda Lyons Kathryn Vincent Stella Egger Linda A Kidambi Usha Stearns Ralph Colletti Adria Teffera Yohannes Tong Sharon Owens Karen Levorse Dorothy Schmidt John A Hagmann William K |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ihor_kopka@merck.com |
| Abstract: | A series of substituted N-(3,5-dichlorobenzenesulfonyl)-(L)-prolyl- and (L)-azetidyl-beta-biaryl beta-alanine derivatives was prepared as selective and potent VLA-4 antagonists. The 2,6-dioxygenated biaryl substitution pattern is important for optimizing potency. Oral bioavailability was variable and may be a result of binding to circulating plasma proteins. |
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