Synthesis and leishmanicidal activity of 2,3,4-substituted-5-imidazolones

Abstract

Twenty-nine imidazolones 1–29 were synthesized and were randomly screened for their in vitro anti-leishmanial potential. Compound 17 showed a good anti-leishmanial activity with an IC₅₀ value of 12.98 ± 0.32 μg/mL. Compounds 14 and 24 were also found to be moderately active (IC₅₀ values 28.20 ± 0.03 and 41.12 ± 0.32 μg/mL, respectively). The activity was compared with that of standard drugs, amphotericin B (IC₅₀ = 0.12 ± 0.41 μg/mL) and pentamidine (IC₅₀ = 2.56 ± 0.10 μg/mL).

Keywords::

• Imidazolone
• substitution effect
• Leishmania major
• leishmanicidal activity

Acknowledgements

This work was financially supported by the Pakistan Telecommunication Company Limited (PTCL) through a research grant (“Synthesis of Leishmanicidal Chemotherapeutic Agents”).

Declaration of interest: The authors report no conflicts of interest.