Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists |
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| Authors: | Ghotas Evindar Sylvie G. Bernier Malcolm J. Kavarana Elisabeth Doyle Jeanine Lorusso Michael S. Kelley Keith Halley Amy Hutchings Albion D. Wright Ashis K. Saha Gerhard Hannig Barry A. Morgan William F. Westlin |
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| Affiliation: | 1. Department of Medicinal Chemistry, Praecis Pharmaceuticals Incorporated, 830 Winter Street, Waltham, MA 02451, USA;2. Department of Preclinical Research, Praecis Pharmaceuticals Incorporated, 830 Winter Street, Waltham, MA 02451, USA |
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| Abstract: | In the design of potent and selective sphingosine-1-phosphate receptor agonists, we were able to identify two series of molecules based on phenylamide and phenylimidazole analogs of FTY-720. Several designed molecules in these scaffolds have demonstrated selectivity for S1P receptor subtype 1 versus 3 and excellent in vivo activity in mouse. Two molecules PPI-4621 (4b) and PPI-4691 (10a), demonstrated dose responsive lymphopenia, when administered orally. |
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