AI Article Synopsis
- The research involved modifying an S1P(1) agonist called AMG 369 to create a new compound that specifically targets S1P(1) while sparing S1P(3) receptors.
- The newly developed compound, named 8c, demonstrated strong effectiveness in reducing blood lymphocyte counts in female Lewis rats when administered orally.
- The results indicate that 8c has favorable pharmacokinetic properties, making it a promising candidate for further studies in drug development.
Article Abstract
Replacement of the azetidine carboxylate of an S1P(1) agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P(3)-sparing S1P(1) agonist, (-)-2-amino-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenyl)-2-methylbutanoic acid (8c), which possessed good in vivo efficacy and pharmacokinetic properties. A 0.3mg/kg oral dose of 8c produced a statistically significant reduction in blood lymphocyte counts 24h post-dosing in female Lewis rats.
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| http://dx.doi.org/10.1016/j.bmcl.2011.12.073 | DOI Listing |
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