Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives |
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| Authors: | dos Santos Maurício S Oliveira Mariana L V Bernardino Alice M R de Léo Rosa M Amaral Veronica F de Carvalho Flavia T Leon Leonor L Canto-Cavalheiro Marilene M |
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| Affiliation: | aDepartamento de Física e Química, Instituto de Ciências Exatas, Universidade Federal de Itajubá, 37500-903 Itajubá, MG, Brazil;bDepartamento de Química Orgânica, Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal Fluminense, 24020-150 Niterói, RJ, Brazil;cLaboratório de Bioquímica de Tripanosomatídeos, IOC, Fundação Oswaldo Cruz, 21040-900 Rio de Janeiro, RJ, Brazil;dDepartamento de Imunobiologia, Instituto de Biologia, Universidade Federal Fluminense, 24020-150 Niterói, RJ, Brazil |
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| Abstract: | ![]()
A series of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (4a–g) and 5-amino-1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (5a–g) were synthesized and evaluated in vitro against three Leishmania species: L. amazonensis, L. braziliensis and L. infantum (L. chagasi syn.). The cytotoxicity was assessed. Among the derivatives examined, six compounds emerged as the most active on promastigotes forms of L. amazonensis with IC50 values ranging from 15 to 60 μM. The reference drug pentamidine presented IC50 = 10 μM. However, these new compounds were less cytotoxic than pentamidine. Based on these results, the more promising derivative 5d was tested further in vivo. This compound showed inhibition of the progression of cutaneous lesions in CBA mice infected with L. amazonensis relative to an untreated control. |
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| Keywords: | Antileishmanial activity Leishmania Azoles Pyrazoles Imidazolines Amidines |
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