Synthesis and leishmanicidal activity of 2,3,4-substituted-5-imidazolones.
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 microg/mL. Compounds 14 and 24 were also found to be moderately active (IC50 values 28.20 +/- 0.03 and 41.12 +/- 0.32 microg/mL, respectively). The activity was compared with that of standard drugs, amphotericin B (IC50 = 0.12 +/- 0.41 microg/mL) and pentamidine (IC50 = 2.56 +/- 0.10 microg/mL).
Khan
Khalid Mohammed
KM
H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan. hassaan2@super.net.pk
Mughal
Uzma Rasool
UR
Ambreen
Nida
N
Samreen
Perveen
Shahnaz
S
Choudhary
M Iqbal
MI
D000666:Amphotericin B / Q000494:pharmacology; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D007891:Leishmania / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D013056:Spectrophotometry, Ultraviolet
D000981:Antiprotozoal Agents; D007093:Imidazoles; D000666:Amphotericin B