865657-31-4Relevant 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.
Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus
Lee, Kyungae,Campbell, Jennifer,Swoboda, Jonathan G.,Cuny, Gregory D.,Walker, Suzanne
supporting information; experimental part, p. 1767 - 1770 (2010/07/08)
A small molecule (1835F03) that inhibits Staphylococcus aureus wall teichoic acid biosynthesis, a proposed antibiotic target, has been discovered. Rapid, parallel, solution-phase synthesis was employed to generate a focused library of analogs, providing detailed information about structure-activity relationships and leading to the identification of targocil, a potent antibiotic.
