title: Synthesis and Antimicrobial Activity of 6-Thioxo-6,7-dihydro-2H-[1,2,4]triazino[2,3-c]-quinazolin-2-one Derivatives.
abstract: Potassium 8-R(1)-9-R(2)-10-R(3)-3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-thiolates 2.1-2.26 were synthesized via cyclocondensation of 6-R-3-(3-R(1)-4-R(2)-5-R(3)-aminophenyl)-1,2,4-triazin-5-ones 1.1-1.26 with carbon disulfide, potassium hydroxide, and ethanol or with potassium O-ethyl dithiocarbonate in 2-propanol. The corresponding thiones 3.1-3.26 were obtained by treatment of 2.1-2.26 with hydrochloric acid. It was found that the nature of the substituents in positions 3, 4, and 5 of the corresponding 6-R-3-(3-R(1)-4-R(2)-5-R(3)-aminophenyl)-1,2,4-triazin-5-ones were affected on the terms of the reaction. The structures of compounds were proven by a complex of physicochemical methods ((1)H, (13)C NMR, LC-MS, and EI-MS). The results of the antibacterial and antifungal activity assay allowed the determination of the high sensitivity of Staphylococcus aureus ATCC 25923 (MIC 6.25-100 μg/mL, MBC 12.5-200 μg/mL) to the synthesized compounds.
authors: Department of Organic and Bioorganic Chemistry, Zaporizhzhia State Medical University, Mayakovsky ave., 26, 69035, Zaporizhzhia, Ukraine.
authors: Inna S
authors: IS
authors: Nosulenko
authors: Department of Organic and Bioorganic Chemistry, Zaporizhzhia State Medical University, Mayakovsky ave., 26, 69035, Zaporizhzhia, Ukraine.
authors: Olexii Yu
authors: OY
authors: Voskoboynik
authors: Department of Pharmacognosy, Pharmaceutical chemistry and Technologies, Department of post-graduate education, Zaporizhzhia State Medical University, Mayakovsky ave., 26, 69035, Zaporizhzhia, Ukraine.
authors: Galina G
authors: GG
authors: Berest
authors: Department of Pharmacy, Crimean State Medical University, 95006, Simferopol, Ukraine.
authors: Sergiy L
authors: SL
authors: Safronyuk
authors: Department of Organic and Bioorganic Chemistry, Zaporizhzhia State Medical University, Mayakovsky ave., 26, 69035, Zaporizhzhia, Ukraine.
authors: Sergiy I
authors: SI
authors: Kovalenko
authors: Department of Microbiology, Virology and Immunology, Zaporizhzhia State Medical University, Mayakovsky ave., 26, 69035, Zaporizhzhia, Ukraine.
authors: Oleksandr M
authors: OM
authors: Kamyshnyi
authors: Department of Microbiology, Virology and Immunology, Zaporizhzhia State Medical University, Mayakovsky ave., 26, 69035, Zaporizhzhia, Ukraine.
authors: Nataliya M
authors: NM
authors: Polishchuk
authors: Department of Organic and Bioorganic Chemistry, Zaporizhzhia State Medical University, Mayakovsky ave., 26, 69035, Zaporizhzhia, Ukraine.
authors: Raisa S
authors: RS
authors: Sinyak
authors: Department of General Chemistry, Crimean State Medical University, 95006, Simferopol, Ukraine.
authors: Andrey V
authors: AV
authors: Katsev
keywords: 6-Thioxo-6,7-dihydro-2H-[1,2,4]triazino[2,3-c]quinazolin-2-one derivatives; Antimicrobial activity; Potassium salt; Synthesis