In continuation of studies on 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine derivatives as 5-HT6 receptor antagonists, new compounds with a pyridine moiety in the 5-and/or 7-position were obtained and their antagonistic activity was screened. It was established that the introduced pyridine changed the 5-HT6 activity. Some of the obtained 5-pyridin-3-yl-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidines 5-HT6 receptor antagonists with K i = 0.2 – 4.5 nM had therapeutic significance for the treatment of some CNS diseases.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 46, No. 7, pp. 19 – 23, July, 2012.
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Ivashchenko, A.V., Golovina, E.S., Kadieva, M.G. et al. Antagonists of serotonin 5-HT6 receptors. III. Pyridine-substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidines: synthesis and structure – activity relationship. Pharm Chem J 46, 406–410 (2012). https://doi.org/10.1007/s11094-012-0810-4
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DOI: https://doi.org/10.1007/s11094-012-0810-4