7-Chloro-4-quinolinyl hydrazones: a promising and potent class of antileishmanial compounds

Chem Biol Drug Des. 2013 May;81(5):658-65. doi: 10.1111/cbdd.12112.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents* / chemical synthesis
  • Antiprotozoal Agents* / chemistry
  • Antiprotozoal Agents* / pharmacology
  • Humans
  • Hydrazones* / chemical synthesis
  • Hydrazones* / chemistry
  • Hydrazones* / pharmacology
  • Leishmania braziliensis / growth & development*
  • Leishmaniasis, Cutaneous / drug therapy*
  • Leishmaniasis, Cutaneous / metabolism
  • Leishmaniasis, Cutaneous / parasitology
  • Macrophages, Peritoneal / metabolism
  • Macrophages, Peritoneal / parasitology*
  • Mice
  • Mice, Inbred BALB C

Substances

  • Antiprotozoal Agents
  • Hydrazones