Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 24, Pages 7451-7454Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.09.134
Keywords
Antileishmanial activity; Leishmania; Azoles; Pyrazoles; Imidazolines; Amidines
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Funding
- Fundacao de Amparo a Pesquisa do Estado do Rio de Janeiro (FAPERJ)
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
- Programa Estrategico de Apoio a Pesquisa em Sa de (PAPES)
- Coordenacao de Aperfeicoamento de Pessoal Docente (CAPES)
- Universidade Federal Fluminense (PROPP-UFF)
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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 mu M. The reference drug pentamidine presented IC50 = 10 mu M. 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. (C) 2011 Elsevier Ltd. All rights reserved.
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