2-Acetylpyridine thiosemicarbazones. 1. A new class of potential antimalarial agents

Abstract

Based on the antimalarial properties seen for 2-acetylpyridine 4-phenyl-3-thiosemicarbazone, 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 contribute to antimalarial activity.