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Novel 4-amino-7-chloroquinoline and [1,2,3]-triazole based hybrids were synthesized in good to excellent yields via Cu[I] catalysed Huisgen 1,3-dipolar cycloaddition of 2-azido-N-(7-chloroquinolin-4-ylaminoalkyl)acetamides with various terminal alkynes in 50% t-butanol in water containing a catalytic amount of CuSO4 and sodium ascorbate at ambient temperature. After spectroscopic characterization, the newly synthesized hybrids were screened for their in vitro antimalarial activity against asexual stages of chloroquine sensitive and chloroquine resistant P. falciparum. Most active compounds were further evaluated for their antimalarial activity against sexual stages (gametocytes) of P. falciparum, the stages responsible for malaria transmission. All compounds demonstrated nanomolar potency against chloroquine sensitive strain (3D7) of P. falciparum. Three lead molecules (8a, 8b and 9c) showing greater potency, when tested against chloroquine resistant field isolate (RKL-9) demonstrated <100 nM IC50 values with 8b showing IC50 of 2.94 nM. Further, compounds (8a, 8b and 9c) were also observed to be causing morphological deformations in mature gametocytes of P. falciparum with IC50 values in micromolar range. Majority of synthesized compounds demonstrated little or no cytotoxicity and exhibited good selectivity indices. Based on our results, these compounds represent ideal candidates for further investigation in terms of their schizonticidal and gametocytocidal potential.
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A protozoan parasite that causes vivax malaria (MALARIA, VIVAX). This species is found almost everywhere malaria is endemic and is the only one that has a range extending into the temperate regions.
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A protozoan parasite that occurs primarily in subtropical and temperate areas. It is the causal agent of quartan malaria. As the parasite grows it exhibits little ameboid activity.
An order of parasitic protozoa found in blood cells and epithelial cells of vertebrates and invertebrates. Life cycles involve both sexual and asexual phases.
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