Abstract:
:In the quest to discover a potent and selective class of direct agonists to the sphingosine-1-phosphate receptor, we explored the carboxylate functional group as a replacement to previously reported lead phosphates. This has led to the discovery of potent and selective direct agonists with moderate to substantial in vivo lymphopenia. The previously reported selectivity enhancing moiety (SEM) and selectivity enhancing orientation (SEO) in the phenylamide and phenylimidazole scaffolds were crucial to obtaining selectivity for S1P receptor subtype 1 over 3.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Evindar G,Deng H,Bernier SG,Doyle E,Lorusso J,Morgan BA,Westlin WFdoi
10.1016/j.bmcl.2012.11.053subject
Has Abstractpub_date
2013-01-15 00:00:00pages
472-5issue
2eissn
0960-894Xissn
1464-3405pii
S0960-894X(12)01505-3journal_volume
23pub_type
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