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Activity of 2-acetylpyridine thiosemicarbazones against Trypanosoma rhodesiense in vitro.

By R A Casero, D L Klayman, G E Childs, J P Scovill and R E Desjardins

Abstract

Twenty-seven 2-acetylpyridine thiosemicarbazones and analogs were tested for antitrypanosomal activity against Trypanosoma rhodesiense using a semiautomated in vitro assay system. Activity was determined by relative inhibition of uptake of two radiolabeled macromolecular precursors, [methyl-3H]thymidine and L-[U-14C]leucine, as compared to untreated controls. It was observed that the nitrogen atom of the pyridyl moiety of the 2-acetylpyridine thiosemicarbazones was essential for antitrypanosomal activity. The 2-acetylpyridine thiosemicarbazones generally inhibited the uptake of L-[U-14C]leucine to a greater extent than they inhibited [methyl-3H]thymidine uptake. Twenty-four of the 27 compounds tested exhibited activity comparable to that found for the antitrypanosomal agent ethidium bromide

Topics: Research Article
Year: 1980
OAI identifier: oai:pubmedcentral.nih.gov:283990
Provided by: PubMed Central
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