AI Article Synopsis
- Selective S1P(4) receptor antagonists could be new treatment options for influenza and help researchers understand how S1P(4) receptors work.
- A promising compound, identified as 5-(2,5-Dichlorophenyl)-N-(2,6-dimethylphenyl)furan-2-carboxamide, was found to effectively target the S1P(4) receptor with moderate potency and high selectivity.
- Further modifications to this compound led to the development of highly selective S1P(4) antagonists that show low nanomolar activity, making them suitable for future optimization studies.
Article Abstract
Selective S1P(4) receptor antagonists could be novel therapeutic agents for the treatment of influenza infection in addition to serving as a useful tool for understanding S1P(4) receptor biological functions. 5-(2,5-Dichlorophenyl)-N-(2,6-dimethylphenyl)furan-2-carboxamide was identified from screening the Molecular Libraries-Small Molecule Repository (MLSMR) collection and selected as a promising S1P(4) antagonist hit with moderate in vitro potency and high selectivity against the other family receptor subtypes (S1P(1-3,5)). Rational chemical modifications of the hit allowed the disclosure of the first reported highly selective S1P(4) antagonists with low nanomolar activity and adequate physicochemical properties suitable for further lead-optimization studies.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3107912 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2011.04.097 | DOI Listing |
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