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N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent,selective VLA-4 antagonists |
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| Authors: | Gutteridge Clare E de Laszlo Stephen E Kamenecka Theodore M McCauley Ermengilda van Riper Gail Mumford Richard A Kidambi Usha Egger Linda A Tong Sharon Hagmann William K |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. gutterid@usna.mil |
| Abstract: | The SAR of 1-sulfonyl-cyclopentyl carboxylic acid amides, ligands for the VLA-4 integrin, was investigated. This effort resulted in the identification of N-(3-phenylsulfonyl-3-piperidinoyl)-(L)-4-(2',6'-dimethoxyphenyl)phenylalanine 52 as a potent, selective VLA-4 antagonist (IC(50)=90 pM). Expansion of the SAR demonstrated that this structural unit can be used to identify a diverse series of sub-nanomolar antagonists. |
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