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Synthesis of square planar complexes for potential antimalarial therapeutics

Vasfi Nejad, Rezvan LU (2024) KEMP30 20232
Department of Chemistry
Abstract
Malaria is an infectious disease that causes death and illness in the world. The effectiveness of antimalarial drugs like chloroquine has decreased, leading to an increase in the use of organometallic complexes to treat malaria. Ferroquine is an organometallic compound that is a newly developed antimalaria drug that contains a 4-aminoquinoline unit that is coordinated to ferrocene. Eight new metal complexes that have the potential to be used as anti-malarial drugs were synthesized and characterized in this study. Two ligands (E)-2-(((2-((6-fluoroquinolin-4-yl)amino)ethyl)imino)methyl)phenol(L1) and (E)-2-(((2-((6-methoxyquinolin-4-yl)amino)ethyl)imino)methyl)phenol that have methoxy- or fluorine at position six of a quinoline moiety were... (More)
Malaria is an infectious disease that causes death and illness in the world. The effectiveness of antimalarial drugs like chloroquine has decreased, leading to an increase in the use of organometallic complexes to treat malaria. Ferroquine is an organometallic compound that is a newly developed antimalaria drug that contains a 4-aminoquinoline unit that is coordinated to ferrocene. Eight new metal complexes that have the potential to be used as anti-malarial drugs were synthesized and characterized in this study. Two ligands (E)-2-(((2-((6-fluoroquinolin-4-yl)amino)ethyl)imino)methyl)phenol(L1) and (E)-2-(((2-((6-methoxyquinolin-4-yl)amino)ethyl)imino)methyl)phenol that have methoxy- or fluorine at position six of a quinoline moiety were synthesized. The ligands were coordinated to platinum, palladium, rhodium, and nickel as bidentate N,O- and N,N-chelaing ligands. Complex 7, N-(2-((2-hydroxyphenyl)methylimino)ethyl)-6- fluoroquinolin-4-amine Rh(I) formed microcrystals. Further research is needed to analyze the new ligands and complexes using different analytical methods, and to evaluate their antimalarial activity. (Less)
Popular Abstract
Malaria is a disease caused by parasites transmitted through mosquito bites, that can often be fatal. The parasites infect the bloodstream and are transferred between humans by mosquitoes. The World Health Organization reported 241 million cases of malaria in 2020, and around 0.6 million of them died. These numbers show that new effective drugs to fight this disease should be found. Quinine is found in the bark of the Cinchona tree and has been used to treat malaria for centuries. Quinine has side effects so scientists created the antimalarial chloroquine in the 1920s, which had lower side effects. New drugs like amodiaquine and 4-aminoquinoline-based drugs were created due to the increase in chloroquine resistance. Chloroquine enters the... (More)
Malaria is a disease caused by parasites transmitted through mosquito bites, that can often be fatal. The parasites infect the bloodstream and are transferred between humans by mosquitoes. The World Health Organization reported 241 million cases of malaria in 2020, and around 0.6 million of them died. These numbers show that new effective drugs to fight this disease should be found. Quinine is found in the bark of the Cinchona tree and has been used to treat malaria for centuries. Quinine has side effects so scientists created the antimalarial chloroquine in the 1920s, which had lower side effects. New drugs like amodiaquine and 4-aminoquinoline-based drugs were created due to the increase in chloroquine resistance. Chloroquine enters the parasite's "digestive vacuole" and stops it from forming a harmful substance. The 4-aminoquinoline needs a structure to be more effective, including a 7-chloro group and a side chain to help it accumulate in the vacuole.
Anti-malaria drugs like chloroquine have become less effective than before due to drug resistance. There is an interest in using metals in chemotherapies so researchers have used metals to find anti-malaria drugs. This research has resulted in the antimalarial drug ferroquine (FQ), which is an organometallic compound that contains a ferrocene molecule that binds to a 4-aminoquinoline and a basic alkylamine. In this study, eight new organometallic compounds with potential as anti-malarial drugs were produced using platinum, palladium, rhodium, and nickel. (Less)
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author
Vasfi Nejad, Rezvan LU
supervisor
organization
course
KEMP30 20232
year
type
L3 - Miscellaneous, Projetcs etc.
subject
keywords
Bioorganometallic chemistry, Malaria, Metal complexes, Platinum-group metals, Synthesis
language
English
id
9150500
date added to LUP
2024-04-04 08:56:15
date last changed
2024-04-04 08:56:15
@misc{9150500,
  abstract     = {{Malaria is an infectious disease that causes death and illness in the world. The effectiveness of antimalarial drugs like chloroquine has decreased, leading to an increase in the use of organometallic complexes to treat malaria. Ferroquine is an organometallic compound that is a newly developed antimalaria drug that contains a 4-aminoquinoline unit that is coordinated to ferrocene. Eight new metal complexes that have the potential to be used as anti-malarial drugs were synthesized and characterized in this study. Two ligands (E)-2-(((2-((6-fluoroquinolin-4-yl)amino)ethyl)imino)methyl)phenol(L1) and (E)-2-(((2-((6-methoxyquinolin-4-yl)amino)ethyl)imino)methyl)phenol that have methoxy- or fluorine at position six of a quinoline moiety were synthesized. The ligands were coordinated to platinum, palladium, rhodium, and nickel as bidentate N,O- and N,N-chelaing ligands. Complex 7, N-(2-((2-hydroxyphenyl)methylimino)ethyl)-6- fluoroquinolin-4-amine Rh(I) formed microcrystals. Further research is needed to analyze the new ligands and complexes using different analytical methods, and to evaluate their antimalarial activity.}},
  author       = {{Vasfi Nejad, Rezvan}},
  language     = {{eng}},
  note         = {{Student Paper}},
  title        = {{Synthesis of square planar complexes for potential antimalarial therapeutics}},
  year         = {{2024}},
}