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Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors |
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| Authors: | Yan Lin Hale Jeffrey J Lynch Christopher L Budhu Richard Gentry Amy Mills Sander G Hajdu Richard Keohane Carol Ann Rosenbach Mark J Milligan James A Shei Gan-Ju Chrebet Gary Bergstrom James Card Deborah Rosen Hugh Mandala Suzanne M |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. lin_yan@merck.com |
| Abstract: | A series of conformationally constrained 3-(N-alkylamino)propylphosphonic acids were systematically synthesized and their activities as S1P receptor agonists were evaluated. Several pyrrolidine and cyclohexane analogs had S1P receptor profiles comparable to the acyclic lead compound, 3-(N-tetradecylamino)propylphosphonic acid (3), lowered circulating lymphocytes in mice after iv administration and were thus identified as being suitable for further investigations. |
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