892296-01-4Relevant academic research and scientific papers
Solution phase parallel synthesis of substituted 3-phenylsulfonyl-[1,2,3] triazolo[1,5- a ]quinazolines: Selective serotonin 5-HT6 receptor antagonists
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.
experimental part, p. 445 - 452 (2010/09/05)
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 i 10 nM in a binding assay, which is 100 times higher than the activity with respect to other serotonin receptors.
