In vitro assessment of 2-acetylpyridine thiosemicarbazones against chloroquine-resistant Plasmodium falciparum.

AUTOR(ES)

Lambros, C

RESUMO

A series of 2-acylpyridine thiosemicarbazones was evaluated in vitro against a chloroquine-resistant Plasmodium falciparum strain. Antimalarial activity was assessed by the inhibition of uptake of [G-3H]hypoxanthine by the parasites. Among the mono- and disubstituted derivatives tested, 13 of 17 had 50% inhibitory doses of less than 10 ng/ml. Increasing the size of the ring at N4 from four to five, six, and seven members produced concomitant decreases in activity. Similarly, increasing the size of the aliphatic substituent on the azomethine carbon reduced activity. Selected compounds were also tested against a chloroquine-susceptible strain. The results suggested that the activities of these agents were not modified significantly by resistance to chloroquine. In general, in vitro activities correlate poorly with the in vivo activities in mice infected with Plasmodium berghei.

Documentos Relacionados

• Antimalarial activities of oligodeoxynucleotide phosphorothioates in chloroquine-resistant Plasmodium falciparum.
• 4-aminoquinoline analogs of chloroquine with shortened side chains retain activity against chloroquine-resistant Plasmodium falciparum.
• In Vitro Potentiation of Antibiotic Activities by a Catecholate Iron Chelator against Chloroquine-Resistant Plasmodium falciparum
• Structure-activity relationships and modes of action of 9-anilinoacridines against chloroquine-resistant Plasmodium falciparum in vitro.
• Chloroquine-resistant P. falciparum infections.