Isosteric ramatroban analogs: Selective and potent CRTH-2 antagonists
The chemoattractant receptor-homologous molecule expressed on T H2 cells (CRTH-2), also found on eosinophils and basophils, is a prostaglandin D2 receptor involved in the recruitment of these cell types during an inflammatory response. In this report, we describe the synthesis and optimization of a ramatroban isostere that is a selective and potent antagonist of CRTH-2 which may be useful in the treatment of certain diseases.
Robarge, Michael J.,Bom, David C.,Tumey, L. Nathan,Varga, Norbert,Gleason, Elizabeth,Silver, Daniel,Song, Jianping,Murphy, Steven M.,Ekema, George,Doucette, Chris,Hanniford, Doug,Palmer, Marc,Pawlowski, Gary,Danzig, Joel,Loftus, Margaret,Hunady, Karen,Sherf, Bruce A.,Mays, Robert W.,Stricker-Krongrad, Alain,Brunden, Kurt R.,Harrington, John J.,Bennani, Youssef L.
p. 1749 - 1753
(2007/10/03)
Potential inhibitors of tyrosine hydroxylase and dopamine-β-hydroxylase
A series of methyl-substituted 1,2,3,4-tetrahydrocarbazoles was synthesized and screened for in vitro activity against tyrosine hydroxylase and dopamine-β-hydroxylase. The most potent compounds were evaluated for inhibition of norepinephrine biosynthesis in rats. The results indicated no significant decrease in norepinephrine levels at three dosage levels.
Scott,Alt,Kemp,Hayes,Telang
p. 1531 - 1535
(2007/10/02)
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