Synthesis of 2-[(ω-phthalimidoalkyl)sulfanyl]- pyrimidin-4(3 H )-ones, their cytotoxicity and in vitro activity against HIV-1/2

The interaction of N -(2-bromoethyl)- and N -(3-bromopropyl)phthalimides with 2-thiouracils substituted at position 6 was studied in alkaline medium, providing S -monoamidoalkylation products and, depending on the substituents, the products of S , O (4)- and S , N (3)-diamidoalkylation. Among the obtained compounds, only 2-[2-(phthalimidoethyl)sulfanyl]-6-(trifluoromethyl)pyrimidin- 4(3 H )-one showed in vitro antiHIV-1 and antiHIV-2 activity at micromolar concentration range.