TAILIEUCHUNG - In vitro anti-BK polyomavirus activity of imidazo[1,2-c]pyrimidine and pyrimido[1,6-a]pyrimidine derivatives

The selectivity index of these compounds is similar to that of cidofovir. Although antiviral activity was evident in secondary assays, significant virus inhibition occurred at or near the cytotoxic concentration (SI90=1). | In vitro anti-BK polyomavirus activity of imidazo 1 2-c pyrimidine and pyrimido 1 6-a pyrimidine derivatives Current Chemistry Letters 9 2020 89 96 Contents lists available at GrowingScience Current Chemistry Letters homepage In vitro anti-BK polyomavirus activity of imidazo 1 2-c pyrimidine and pyrimido 1 6-a pyrimidine derivatives Roman Solomyannyia Oleg Mitiukhina Mark Prichardb Scott Jamesb Carol Hartlineb Victor Zhirnova and Volodymyr Brovaretsa a Department of Chemistry of Bioactive Nitrogen-Containing Heterocyclic Bases . Kukhar Institute of Bioorganic Chemistry and Petrochemistry NAS of Ukraine 1 Murmanska str Kyiv 02094 Ukraine b Department of Pediatrics University of Alabama at Birmingham Birmingham Alabama 35233 United States CHRONICLE ABSTRACT Article history Five imidazo 1 2-c pyrimidine and pyrimido 1 6-a pyrimidine derivatives were designed Received August 1 2019 synthesized and evaluated for their antiproliferative activity and cytotoxicity. Primary Received in revised form bioassays in vitro showed that two of five synthesized compounds 6-benzyl-8- August 18 2019 methylsulfonyl -2 6-dihydroimidazo 1 2-c pyrimidin-5 3H -one and 9- methylsulfonyl -7- Accepted September 16 2019 propyl-2 3 4 7-tetrahydro-6H-pyrimido 1 6-a pyrimidin-6-one possessed potent antiviral Available online activity against BKV EC50 μM and respectively . The selectivity index of these September 16 2019 compounds is similar to that of cidofovir. Although antiviral activity was evident in secondary Keywords assays significant virus inhibition occurred at or near the cytotoxic concentration SI90 1 . Antiviral activity Pyrimidine derivatives Here we show that substituted pyrimidine derivatives are a promising structure class of BK polyomavirus chemical compounds for the development of antiviral drugs against BKV infections. Hence Heterocycles these compounds may be taken as lead compounds for further development of novel Cyclization .

• Hoá học
• Vitro anti BK polyomavirus activity
• imidazo [1
• 2 c] pyrimidine
• pyrimido [1
• 6 a] pyrimidine derivatives
• Substituted pyrimidine derivatives
• Antiviral drugs against BKV infections