SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF PHENYLSELENYL
TRIBROMIDE AND ITS FUSED THIENOPYRIMIDINE DERIVATIVES
BORIS M. SHARGA1*, ANDRIJ O. KRIVOVJAZ1, MIKHAILO V. SLIVKA1, LARISA M. LAMBRUCH2, ANTONINA V. CHEYPESH2, VASIL G. LENDEL1, VITALY I. NIKOLAYCHUK1, VLADIMIR P. MARKOVICH2
1Uzhgorod National University, 3 Narodna Sq., 88000, Uzhgorod, Ukraine
2Regional Station of Sanitary and Epidemiology, 96 Sobranеtska Str., 88000, Uzhgorod, Ukraine
*corresponding author: bmsharga@yahoo.co.uk
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Abstract:
Fused thienopyrimidine derivatives of phenylselenyl tribromide (compound III) were synthesized and characterized by
spectral and elemental analyses. The parental compound and its derivatives were tested in vitro for their antimicrobial
activity. The minimum inhibitory (bacteriostatic or fungistatic) concentrations and minimum bactericidal or fungicidal
concentrations were estimated for the two most active compounds: 1-bromо-2-[(E)-1-bromomethyliden]-1,5-diphenyl-6-oxo-
2,3,5,6,7,8,9,10-octahydrobenzo[b]thieno[3',2',5,6]pyrimido-[2,1-b][1,4,3] thiaselenazin-12-ium bromide (compound IVc),
the derivative with the lowest toxicity, and phenylselenyl tribromide (compound III), the starting chemical with the highest
toxicity. These two compounds yielded mainly bactericidal effects on the tested bacteria. In comparison with the minimum
bactericidal concentrations of cefotaxime, this effect was significantly weaker. Of the two afore-mentioned compounds, only
the derivative IVc demonstrated fungicidal action against yeasts. In comparison with the minimum fungistatic concentrations
of fluconazole, the inhibitory potency of this compound against yeasts was two times stronger. The compound manifested
fungicidal effects against yeasts at doses of 275 - 310 μg/mL, while fluconazole yielded only fungistatic actions. Among the
studied compounds, ІІI and IVc appear to be most active against yeasts and also possess poor to moderate activity against
Gram-positive and Gram-negative bacteria. The antibacterial activity can be improved by introducing changes into the
chemical structure of the compounds. Considering the obtained results, these products and their derivatives may be of
practical benefit.






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