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• W2907662009 abstract "Abstract Novel 4‐amino‐7‐chloroquinoline‐based 1,2,3‐triazole hybrids were synthesised in good yields by Cu I ‐catalysed Huisgen 1,3‐dipolar cycloaddition reactions of 2‐azido‐ N ‐(7‐chloroquinolin‐4‐ylaminoalkyl)acetamides with various terminal alkynes. These new hybrids were screened in vitro against asexual blood stages of the chloroquine‐sensitive 3D7 strain of P. falciparum . The most active compounds were further screened against asexual and sexual stages (gametocytes) of the chloroquine‐resistant RKL‐9 strain of P. falciparum . Although all compounds were less potent than chloroquine against the 3D7 strain, the three best compounds were appreciably more active than chloroquine against the RKL‐9 strain, displaying IC 50 values of <100 n m , with one of them having an IC 50 of 2.94 n m . Further, the lead compounds were gametocytocidal with IC 50 values in the micromolar range, and were observed to induce morphological deformations in mature gametocytes. Most compounds demonstrated little or no cytotoxicity and exhibited good selectivity indices. The most active compounds represent promising candidates for further evaluation of their schizonticidal and gametocytocidal potential." @default.
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• W2907662009 date "2019-01-29" @default.
• W2907662009 modified "2023-10-18" @default.
• W2907662009 title "Targeting Asexual and Sexual Blood Stages of the Human Malaria Parasite <i>P. falciparum</i> with 7‐Chloroquinoline‐Based 1,2,3‐Triazoles" @default.
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• W2907662009 doi "https://doi.org/10.1002/cmdc.201800728" @default.
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