Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.

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.

journal_name

Bioorg Med Chem Lett

authors

Evindar G,Bernier SG,Kavarana MJ,Doyle E,Lorusso J,Kelley MS,Halley K,Hutchings A,Wright AD,Saha AK,Hannig G,Morgan BA,Westlin WF

doi

10.1016/j.bmcl.2008.11.072

subject

Has Abstract

pub_date

2009-01-15 00:00:00

pages

369-72

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01458-3

journal_volume

19

pub_type

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