7‐Chloro‐4‐quinolinyl Hydrazones: A Promising and Potent Class of Antileishmanial Compounds |
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| Authors: | Elaine S Coimbra Luciana M R Antinarelli Adilson D da Silva Marcelle L F Bispo Carlos R Kaiser Marcus V N de Souza |
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| Affiliation: | 1. Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Cidade Universitária, , 36036‐900 Juiz de Fora, MG, Brazil;2. Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Cidade Universitária, , Juiz de Fora, MG, Brazil;3. Funda??o Oswaldo Cruz, Instituto de Tecnologia em Fármacos‐Far Manguinhos, , 21041‐250 Rio de Janeiro, RJ, Brazil;4. Departamento de Química Organica, Instituto de Química, Universidade Federal do Rio de Janeiro, , Rio de Janeiro, RJ, Brazil |
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| Abstract: | In this work, we report the antileishmanial evaluation of twenty 7‐chloro‐4‐quinolinyl hydrazone derivatives ( 1 – 20 ). Firstly, the compounds were tested against promastigotes of four different Leishmania species. After that, all derivatives were assayed against L. braziliensis amastigotes and murine macrophages. Furthermore, it was investigated whether the antiamastigote L. braziliensis effect of the compounds could be associated with nitric oxide production. Compounds 6 and 7 showed a strong leishmanicidal activity against intracellular parasite with IC50 in nanogram levels (30 and 20 ng/mL, respectively). Appreciable activity of three compounds tested can be considered an important finding for the rational design of new leads for antileishmanial compounds. |
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| Keywords: | 7‐chloro‐4‐quinolinyl hydrazones amodiaquine antileishmanial |
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