Synthesis and In Vitro Leishmanicidal Effects of Conformationally Restricted Analogues of Pentamidine

Author(s):
Farzin HadizadehFarzin Hadizadeh1, 2,*, Mahmoud Reza JaafariMahmoud Reza Jaafari1, 2, Afshin SamieiAfshin Samiei2, Azam MostafaviradAzam Mostafavirad1, Ebrahim MohammadianEbrahim Mohammadian2
1Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
2Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran
*Corresponding Author: Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran. Email:[email protected]

IJ Pharmaceutical Research:Vol. 8, issue 4; 257-262
Published online:Nov 20, 2010
Article type:Research Article
Received:Nov 01, 2008
Accepted:Jun 01, 2009
How to Cite:Hadizadeh F, Jaafari MR, Samiei A, Mostafavirad A, Mohammadian E. Synthesis and In Vitro Leishmanicidal Effects of Conformationally Restricted Analogues of Pentamidine. Iran J Pharm Res. 2022;8(4):e128646. doi: https://doi.org/10.22037/ijpr.2010.819

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 solvent had no significant effect on L. major promastigotes. All compounds had significant effect compared to DMSO and were less potent than positive controls.

Copyright

© 2022, Author(s). This open-access article is available under the Creative Commons Attribution 4.0 (CC BY 4.0) International License (https://creativecommons.org/licenses/by/4.0/), which allows for unrestricted use, distribution, and reproduction in any medium, provided that the original work is properly cited.

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