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SYNTHESIS OF 2-[(ω-PHTHALIMIDOALKYL)SULFANYL]PYRIMIDIN-4(3H)-ONES, THEIR CYTOTOXICITY AND in vitro ACTIVITY AGAINST HIV-1/2

Иван А. Новаков, Дмитрий С. Шейкин, Виктор В. Чапуркин, Максим Б. Навроцкий, Александр С. Бабушкин, Ярослав П. Кузнецов, Евсей А. Ручко, Вадим В. Качала, Антон Ю. Марышев, Доминик Шольц
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Abstract


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(3H)-one showed in vitro antiHIV-1 and antiHIV-2 activity at micromolar concentration range.

 


Keywords


2-thiouracil; uracil; phthalimidoalkylation; antiHIV-1/2 activity; antiviral activity.

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