2-Acetylpyridine thiosemicarbazones. 1. A new class of potential antimalarial agents.
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.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000627:therapeutic use; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use
D000962:Antimalarials; D011725:Pyridines; D013882:Thiosemicarbazones