Author/Authors :
Hadizadeh, Farzin Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad , Jaafari, Mahmoud Reza Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad , Mostafavirad, Azam Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad , Samiei, Afshin Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad , Mohammadian, Ebrahim Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad
Abstract :
Four conformationally restricted analogues of pentamidine were prepared. Then, different
concentrations (0.039, 0.078, 0.156, 0.312 and 0.625 mg/mL) of each compound and two
positive controls (amphotericin B and pentamidine, 0.625 mg/mL), one negative control
(culture medium) and one solvent control (DMSO) were prepared and placed in 24-well plates
containing 50000 parasite per well. Promastigotes of Leishmania major were incubated over
a period of 2 days at 25°C; subsequently, percent of viable parasite in each well determined
spectrophotometrically using MTT assay. The average EC50 for compounds 4a,b and 8a,b in
DMSO was 0.098, 0.410, 0.150, 0.720 mg/mL, respectively. The average EC50 for positive
controls pentamidine and amphotericin B was found to be 0.062 and 0.026 mg/mL. The control
effect compared to DMSO and were less potent than positive controls
Keywords :
Conformationally restricted , Pentamidine , Analogues , Leishmaniasis , Introduction Protozoal parasitic
