期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 12, 页码 2544-2552出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00536
关键词
Plasmodium falciparum; 4-aminoquinolines; 1,8-naphthalic anhydride; dual function antiplasmodial; hemozoin inhibition; PfCRT
资金
- Department of Science and Technology (DST), New Delhi, India [IF160180]
- Direction Generale pour l'Armement [PDH-2-NRBC-4-B-4104]
- National Research Foundation (NRF) South Africa [121276]
A series of amide tethered 4-aminoquinoline-naphthalimide hybrids has been synthesized to assess their in vitro antiplasmodial potential against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The most active and noncytotoxic compound had an IC50 value of 0.07 mu M against W2 strain and was more active than standard antimalarial drugs, including chloroquine, desethylamodiaquine, and quinine, particularly for drug resistant malaria. The promising scaffold, when subjected to heme binding and molecular modeling studies, was identified as a possible potent inhibitor of hemozoin formation and P. falciparum chloroquine resistance transporter (PfCRT), respectively, and, therefore, could act as a dual function antiplasmodial.
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