Novel azoles with potent antileishmanial activity

Future Microbiol. 2021 Aug:16:871-877. doi: 10.2217/fmb-2020-0320. Epub 2021 Jul 28.

Abstract

Aim: To investigate the antileishmanial activity of novel azole compounds against Leishmania donovani, which causes deadly visceral leishmaniasis disease. Materials & methods: A focused azole-based library was screened against both promastigotes and amastigotes forms of L. donovani strains in flat-bottomed 96-well tissue culture plates and J774A.1 macrophage cell-line infected with L. donovani. The comprehensive screening of azole-based library against L. donovani strains provided novel hits, which can serve as a good starting point to initiate hit to lead optimization campaign. Results: Hits identified from azole-based library exhibited potent in vitro activity against promastigotes and amastigotes of L. donovani. Conclusion: These potent novel azole hits could be a good starting point to carry out for further medicinal chemistry exploration for antileishmania program.

Keywords: Leishmania donovani; amatigotes; azoles; promastigotes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Azoles* / pharmacology
  • Cell Line
  • Leishmania donovani* / drug effects
  • Macrophages / parasitology
  • Mice

Substances

  • Azoles