7-Chloro-4-quinolinyl hydrazones: a promising and potent class of antileishmanial compounds.
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.
Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, MG, Brazil.
Elaine S
ES
Coimbra
Luciana M R
LM
Antinarelli
Adilson D
AD
da Silva
Marcelle L F
ML
Bispo
Carlos R
CR
Kaiser
Marcus V N
MV
de Souza
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007892:Leishmania braziliensis / Q000254:growth & development*; D016773:Leishmaniasis, Cutaneous / Q000188:drug therapy* / Q000378:metabolism / Q000469:parasitology; D017737:Macrophages, Peritoneal / Q000378:metabolism / Q000469:parasitology*; D051379:Mice; D008807:Mice, Inbred BALB C
D000981:Antiprotozoal Agents; D006835:Hydrazones