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  • Title: Selective leishmanicidal effect of 1,3,4-thiadiazole derivatives and possible mechanism of action against Leishmania species.
    Author: Poorrajab F, Ardestani SK, Foroumadi A, Emami S, Kariminia A, Behrouzi-Fardmoghadam M, Shafiee A.
    Journal: Exp Parasitol; 2009 Apr; 121(4):323-30. PubMed ID: 19124020.
    Abstract:
    With the aim of determining selectivity and the possible target(s) of nitroheteroaryl-1,3,4-thiadiazoles considered as possible leads for the development of anti-leishmanial agents, we studied 5-nitroimidazole, 5-nitrofuran and 5-nitrothiophene analogs of N-substituted-piperazinyl-1,3,4-thiadiazoles. We investigated 21 representative compounds 1-3(a-g) for the following properties: selectivity and efficiency against different Leishmania wild type species and intracellular parasite, toxicity against host cells and inhibition of topoisomerases I and II. Our results indicate that the nitroimidazole analogs 1a and 1f, and nitrofuran derivatives 2a, 2b, 2c, 2f, and 2g exhibited low toxicity against the host cells (IC(50)> or =80 microM), but high selectivity against intracellular amastigotes (selectivity index>12). Leishmania topoisomerases revealed impressive sensitivity to the agents (%inhibition >50 at IC(50) doses of compounds against Leishmania). Our findings showed that at least part of leishmaniacidal effect of the compounds could be attributed to disruption DNA-relaxed activities of topoisomerases I and II, and cleavable-complex formation.
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