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N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists |
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| Authors: | Yang Ginger X Chang Linda L Truong Quang Doherty George A Magriotis Plato A de Laszlo Stephen E Li Bing MacCoss Malcolm Kidambi Usha Egger Linda A McCauley Ermengilda Van Riper Gail Mumford Richard A Schmidt John A Hagmann William K |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ginger_yang@merck.com |
| Abstract: | Given the proposed involvement of VLA-4 in inflammatory processes, a program to identify orally active VLA-4 antagonists was initiated. Herein, we report the discovery of a N-tetrahydrofuroyl-(L)-phenylalanine derivative (17) and related analogues as potent VLA-4 antagonists with good oral bioavailability. |
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