Targeting Asexual and Sexual Blood Stages of the Human Malaria Parasite P. falciparum with 7‐Chloroquinoline‐Based 1,2,3‐Triazoles
Novel 4‐amino‐7‐chloroquinoline‐based 1,2,3‐triazole hybrids were synthesised in good yields by CuI‐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 b...
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Veröffentlicht in: | ChemMedChem 2019-02, Vol.14 (4), p.484-493 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Novel 4‐amino‐7‐chloroquinoline‐based 1,2,3‐triazole hybrids were synthesised in good yields by CuI‐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 IC50 values of |
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ISSN: | 1860-7179 1860-7187 |
DOI: | 10.1002/cmdc.201800728 |