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N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists |
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| Authors: | Li Bing de Laszlo Stephen E Kamenecka Theodore M Kopka Ihor E Durette Philippe L Lanza Thomas MacCoss Malcolm Tong Sharon Mumford Richard A McCauley Ermengilda D Van Riper Gail Schmidt John A Hagmann William K |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. bing_li@merck.com |
| Abstract: | A series of potent N-(aralkyl-, arylcycloalkyl-, and heteroaryl-acyl)-4-biphenylalanine VLA-4 antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further optimization led to several highly potent compounds (IC(50) <1 nM). Evaluation of rat pharmacokinetic revealed generally high clearance. |
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