AI Article Synopsis
- - The study investigated how changes to sphingosine-1-phosphate (S1P) receptor agonists affect their activity and selectivity.
- - A modified cinnamyl derivative was developed to boost its effectiveness on the S1P(1) receptor while ensuring it does not activate the S1P(3) receptor.
- - Derivative 10d was recognized as a strong S1P(1) agonist, showing great selectivity against the S1P(3) receptor, and effectively reducing lymphocyte levels in mice.
Article Abstract
Structure-activity relationship of sphingosine-1-phosphate receptor agonists was examined. Cinnamyl derivative 1 was modified to improve S1P(1) agonistic activity as well as selectivity over S1P(3) agonistic activity. Dihydronaphthalene derivative 10d was identified as a potent S1P(1) receptor agonist with high selectivity against S1P(3) and enhanced efficacy in lowering peripheral lymphocyte counts in mice.
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| http://dx.doi.org/10.1016/j.bmcl.2011.05.029 | DOI Listing |
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