Antileishmanial activity of benzocycloalkyl azole oximino ethers: the conformationally constraint analogues of oxiconazole

Acta Trop. 2011 Feb;117(2):157-60. doi: 10.1016/j.actatropica.2010.10.011. Epub 2010 Nov 13.

Abstract

Antileishmanial activities of 16 synthetic oximino benzocycloalkyl azoles against Leishmania donovani were evaluated in vitro against extracellular promastigotes and intracellular amastigotes. Based on SI (Selectivity Index), five compounds were tested further in vivo in hamster model. Out of these, three compounds have shown medium activity (53-58%) and one has shown significant inhibition of parasite multiplication (70%). Despite the fact that these compounds were better than the existing antileishmanials in respect to IC(50) and SI values, they were less active than miltefosine in vivo. The present study has helped us in identifying a new lead that could be exploited as a potential antileishmanial agent.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiparasitic Agents / chemical synthesis
  • Antiparasitic Agents / chemistry
  • Antiparasitic Agents / pharmacology*
  • Cricetinae
  • Disease Models, Animal
  • Ethers / chemical synthesis
  • Ethers / chemistry
  • Ethers / pharmacology*
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Leishmania donovani / drug effects*
  • Leishmaniasis, Visceral / drug therapy*
  • Lethal Dose 50

Substances

  • Antiparasitic Agents
  • Ethers
  • Imidazoles
  • oxiconazole