SYNTHESIS AND IN VITRO LEISHMANICIDAL AND CYTOTOXIC ACTIVITIES OF 2-STYRYLQUINOLINES ANALOGS
The search of new treatments for leishmaniasis is an active task nowadays, since there is a lack of nontoxic, cheap and non-resistant medication. In the literature several quinolines have shown in vitro activity against agents of cutaneous leishmaniasis, visceral leishmaniasis, African trypanosomias...
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| Autores principales: | , , , , , , |
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| Formato: | article |
| Lenguaje: | EN |
| Publicado: |
Universidad de Antioquia
2009
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| Materias: | |
| Acceso en línea: | https://doaj.org/article/07fca273a0614aeaa1e63f3e0f7779c7 |
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| Sumario: | The search of new treatments for leishmaniasis is an active task nowadays, since there is a lack of nontoxic,
cheap and non-resistant medication. In the literature several quinolines have shown in vitro activity
against agents of cutaneous leishmaniasis, visceral leishmaniasis, African trypanosomiasis and Chagas
diseases. Six 2-styrylquinolines derived from galipeine were synthesized by Perkin condensation of
quinaldine with aromatic aldehydes. Leishmanicidal activity was estimated for Leishmania panamensis at the amastigote form and cytotoxic activity against U-937 cells. All compounds showed activity against
both L. panamensis and U-937 cells. (E)-2-(2,5-dimethoxyphenyl)ethenyl)quinoline (1), (E)-2-(2,3-
dimethoxyphenyl)ethenyl)quinoline (2) and (E)-N-[4-(2-quinolin-2-yl-ethenyl)phenyl]acetamide (3)
were more active against axenic (EC50= 3.7, 4.5 and 19.1μg/mL) and intracellular amastigotes (EC50=
1.4, 1.8 and 1.7μg/ml, respectively), in comparison with hydrogenated derivatives 2-[2-(2,5-dimethoxy
phenyl)ethyl]quinoline (1a), 2-[2-(2,3-dimethoxyphenyl)ethyl]quinoline (2a) and N-[4-(2-quinolin-
2-ylethyl)phenyl]acetamide (3a) (CE50= 31.1, 23.6 and 59.3μg/mL, respectively). All compounds were
also active against the U-937 cells. Styrylquinolines 1, 2 and 3 showed a LC50 of 3.7, 6.2 and 4.5μg/mL,
respectively and the hydrogenated derivatives 1a, 2a and 3a showed a LC50 of 16.0. 12.9 and 20.2μg/mL,
respectively. Although hydrogenation reduced the leishmanicidal and cytotoxic activities, the activity
showed against Leishmania parasites suggests this compound series has potential as drug candidates for
the treatment of leishmaniasis.
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