| Autor: |
Suh, Y.-G., Lee, Y.-S., Min, K.-H., Park, O.-H., Kim, J.-K., Seung, H.-S., Seo, S.-Y., Lee, B.-Y., Nam, Y.-H., Lee, K.-O., Kim, H.-D., Park, H.-G., Lee, J., Oh, U., Lim, J.-O., Kang, S.-U., Kil, M.-J., Koo, J.-y., Shin, S. S., Joo, Y.-H., Kim, J. K., Jeong, Y.-S., Kim, S.-Y., Park, Y.-H. |
| Zdroj: |
Journal of Medicinal Chemistry; September 2005, Vol. 48 Issue: 18 p5823-5836, 14p |
| Abstrakt: |
Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure−activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure−activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca2+ uptake inhibition in rat DRG neuron with IC50 between 10 and 100 nM. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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