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Ultrasound-assisted synthesis and structure elucidation of novel quinoline-pyrazolo1,5-apyrimidine hybrids for anti-malarial potential against drug-sensitive and drug-resistant malaria parasites and molecular docking
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Ultrasound-assisted synthesis and structure elucidation of novel quinoline-pyrazolo1,5-apyrimidine hybrids for anti-malarial potential against drug-sensitive and drug-resistant malaria parasites and molecular docking
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Ultrasound-assisted synthesis and structure elucidation of novel quinoline-pyrazolo1,5-apyrimidine hybrids for anti-malarial potential against drug-sensitive and drug-resistant malaria parasites and molecular docking
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Journal Article
Ultrasound-assisted synthesis and structure elucidation of novel quinoline-pyrazolo1,5-apyrimidine hybrids for anti-malarial potential against drug-sensitive and drug-resistant malaria parasites and molecular docking
2024
Overview
Novel
(E)
-3-(dimethylamino)-1-(quinolin-3-yl)prop-2-en-1-one and
(E)
-3-(dimethylamino)-1-(quinolin-3-yl)but-2-en-1-one
(2)
were synthesized in excellent yields by reacting 3-acetylquinoline with DMF-DMA and DMA-DMA respectively. Subsequently,
2
were used as the precursors for the synthesis of 3-(pyrazolo[1,5-
a
]pyrimidin-7-yl)quinolines and 3-(5-methylpyrazolo[1,5-
a
]pyrimidin-7-yl)quinolines (
4
). All the synthesized compounds were subjected to structure elucidation and evaluated for their antiparasitic potential with special reference to their anti-malarial properties. The
in-vitro
studies of the synthesized compounds revealed moderate anti-malarial efficacy for compounds
4b
,
4c
,
4d
,
4k
,
4l
and
4m
. Compounds
4g
and
4i
showed highest activity displaying IC
50
values of 2.10 and 2.77
μ
M, respectively, for the chloroquine-sensitive strain of
P
. falciparum, and 4.26 and 2.87
μ
M, respectively, for the chloroquine-resistant strain. The
in-vitro
cytotoxicity of the compounds showed CC
50
as >500
µ
M and thus, found to be safe. Molecular docking of the novel series of ligand
4a
–
4n
against the target protein
P. falciparum Pf
LDH enzyme target (PDB ID 1LDG) revealed good binding energies ranging from –8.06 to –11.02 kcal/mol with low inhibition constants summed up as 1.04, 473.55, 352.51, 290.9, 437.86, 1.23, 41.18, 26.81, 162.76, 300.38, 70.2, 29.84, 4.14, 8.4
µ
M, respectively. The lower the inhibition constant (
µ
M), the greater is the binding affinity and lower the medication required to inhibit the activity of the target receptor.
Graphical abstract
(E)
-3-(dimethylamino)-1-(quinolin-3-yl)but-2-en-1-one with 3-aminopyrazole under ultrasonic irradiation in aqueous medium yielded novel 3-(pyrazolo[1,5-
a
]pyrimidin-7-yl)quinolines and 3-(5-methylpyrazolo[1,5-
a
]pyrimidin-7-yl)quinolines. Antimalarial studies against
Pf
3D7 strain resulted in moderate activity with compound
4g
showing highest activity. Molecular docking analysis of the compounds reveals the potentiality of the series to serve as antimalarial agents against CQ-sensitive (
Pf
3D7) and multi-drug-resistant (
Pf
K1).
Publisher
Springer India,Springer Nature B.V
Subject
