
Journal of Combinatorial Chemistry p. 445 - 452 (2010)
Update date:2022-08-05
Topics:
Ivachtchenko, Alexandre V.
Golovina, Elena S.
Kadieva, Madina G.
Koryakova, Angela G.
Kovalenko, Sergiy M.
Mitkin, Oleg D.
Okun, Ilya M.
Ravnyeyko, Irina M.
Tkachenko, Sergey E.
Zaremba, Oleg V.
Here we present the solution phase parallel synthesis of a combinatorial library consisting of 776 new substituted 3-phenylsulfonyl-[1,2,3]triazolo[1,5- a]quinazolines and a study of the relation of their structure with a 5-HT 6 receptor antagonistic activity in a functional cell (HEK 293) analysis and radioligand competitive binding. We have found highly active and selective 5-HT6R antagonists. The most active 5-HT6R antagonists have IC50 <100 nM in a functional assay, and K i <10 nM in a binding assay, which is 100 times higher than the activity with respect to other serotonin receptors.
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