Synthesis and biological study of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines as potent and selective serotonin 5-HT6 receptor antagonists |
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| Authors: | Alexandre V. Ivachtchenko Elena S. Golovina Madina G. Kadieva Angela G. Koryakova Sergiy M. Kovalenko Oleg D. Mitkin Ilya M. Okun Irina M. Ravnyeyko Sergey E. Tkachenko Oleg V. Zaremba |
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| Affiliation: | 1. Chemical Diversity Research Institute, 114401 Khimki, Moscow Reg, Russia;2. ChemDiv, Inc., 6605 Nancy Ridge Drive, San Diego, CA 92121, USA;3. Institute of Combinatorial Organic Chemistry, Kharkiv, Ukraine;4. National Pharmaceutical University, Kharkiv, Ukraine |
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| Abstract: | A number of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines were prepared and their 5-HT6 receptor binding affinity and ability to inhibit the functional cellular responses to serotonin were evaluated. 3-[(3-Chlorophenyl)sulfonyl]-N-(tetrahydrofuran-2-ylmethyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidin-5-amine 2{5,26} appeared to be the most active in a functional assay (IC50 = 29.0 nM) and 3-(phenylsulfonyl)-N-(2-thienylmethyl) thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidin-5-amine 2{1,28} demonstrated the greatest affinity in a 5-HT6 receptor radioligand binding assay (Ki = 1.7 nM). A screening of 5-HT2A and 5-HT2B receptor affinity revealed that 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines are highly selective 5-HT6 receptor ligands. |
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