Based on the antimalarial properties observed for 2-acetylpyridine 4-phenyl-3-thiosemicarbazone (1), an extensive series of related thiosemicarbazones was prepared and tested against Plasmodium berghei in mice. Screening results indicated that the presence of the 2-pyridylethylidene group was critical and that certain phenyl, benzyl, phenethyl, or cycloalkyl groups at N4 of the thiosemicarbazone moiety also contribute to antimalarial activity.
Elemental powdered selenium and sodium borohydride react very readily in water or ethanol to give either sodium hydrogen selenide or sodium diselenide, depending on the ratio of the reactants. The sodium hydrogen selenide and sodium diselenide solutions, thus prepared, can be utilized directly in typical nucleophilic displacement reactions. Alkali metal borohydrides have been combined l with the chalcogen elements by direct fusion1•2 and in aprotic solvents such as ether,2 dioxane,8 tetrahydrofuran,4•5 and diglyme.4•5 Under the latter conditions, sulfur, selenium, and tellurium were incorporated directly into the borohydride.4•5 The product of the reaction between selenium and sodium borohydride
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