Synthesis and Comparison of Anti-Leishmania major Activity of Antimony and Iron Complexes of 3-Hydroxypyran-4-One and 3-Hydroxypyridine-4- One as Bi-Dentate Ligands

Author(s):
Zeynab ZarrabiZeynab Zarrabi1, Latfollah SaghaieLatfollah Saghaie1, Afshin FassihiAfshin Fassihi1, Nader PestechianNader Pestechian2, Sedigheh SaberiSedigheh SaberiSedigheh Saberi ORCID2,*
1Department of Medicinal Chemistry and Isfahan Pharmaceutical Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
2Department of Mycology and Parasitology, School of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran
*Corresponding Author: Corresponding author: Department of Mycology and Parasitology, School of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran. Email:[email protected]

Journal of Reports in Pharmaceutical Sciences:Vol. 9, issue 2; 177-82
Published online:Oct 07, 2020
Article type:Research Article
Received:Nov 24, 2018
Accepted:Dec 03, 2018
How to Cite:Zarrabi Z, Saghaie L, Fassihi A, Pestechian N, Saberi S. Synthesis and Comparison of Anti-Leishmania major Activity of Antimony and Iron Complexes of 3-Hydroxypyran-4-One and 3-Hydroxypyridine-4- One as Bi-Dentate Ligands. J Rep Pharm Sci. 2020;9(2):e147110. doi: https://doi.org/10.4103/jrptps.JRPTPS_64_18

Abstract

Background: Leishmaniasis infection threatens millions of people in under developing and developing countries. Treatment of this neglected disease is very complicated.
Subjects and Methods: A novel series of antimony (V) complexes using bidentate ligands of hydroxypyranones and hydroxypyridinones have been designed and synthesized. For the synthesis of the complexes, SbCl5 in water was added to the solution of each ligand at 60°C and the pH of mixture was adjusted to 8 using aqueous NaOH. After 24 h stirring, extraction of produced compound into acetone gave the desired complex. The structure of complexes was achieved by using FTIR, 1HNMR, and electron spin ionization mass spectroscopic techniques. All compounds were evaluated for in vitro anti amastogote form of Leishmania major. 
Results and Conclusion: The most potent antimony complexes against amastigotes were 5b (after 48 and 72 h) and 5a (after 72 h) with IC50 values of 24.4, 16.3, and 30.1 μg/mL, respectively. Furthermore, antimony and iron complexes were used together for in vitro anti amastigote form of L. major activity. These compounds were toxic for macrophages and destroyed them. 
 

Copyright

© 2020, 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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