Antimalarial activity of HIV-1 protease inhibitor in chromone series

Antimalarial and β-hematin formation inhibitory activities of chromone derivatives

“…The chromone compounds used in this study were available from previous works and were prepared as described in the report of those studies 19,20 .…”

“…In our previous study, we have reported the antimalarial activity against P. falciparum (K1, multidrug resistant strain) of twenty-one chromone compounds using microculture radioisotope assay 20 . In this study, a series of more than 21 compounds were tested using the same method.…”

“…Compounds 3,4,23,24,27,36,38, and 43 in Group I displayed highly potent antimalarial activity (IC 50 0.95-19.66 µM) and β-hematin formation inhibitory activity (IC 50 1.41-30.56 µM). In group II, compounds 11,13,16,17,20,34,37, 39, 44-50 showed potent antimalarial activity (IC 50 3.82-14.69 µM) but they possessed low β-hematin formation inhibition (less than 45% inhibition). On the other hand, compounds 25, 26, 28, and 42 in Group III were potent β-hematin formation inhibitor (IC 50 2.30, 2.54, 3.69, and 24.01 µM, respectively) but weak as antimalarial drug (less than 40% inhibition).…”

New paradigm of an old target: An update on structural biology and current progress in drug design towards plasmepsin II

“…piperazin-1-yl] propan-1-ol showed high inhibitory activity on P.falciparum (IC 50 =0.5µM) antimalarial activity was due to combined existence of a hydroxyl group, a propane chain and a fluorine(76). Molecular docking studies and electrostatic calculation displayed that this inhibitor could bind to the Plm II active site.…”

Heteroannulated Coumarins and Chromones from Chemical Transformations of 6,8‐Dimethylchromone‐3‐carbonitrile

“…Due to their abundance in plants and their low mammalian toxicity, chromone derivatives are existing in large amounts in the diet of humans . Chromone derivatives revealed a wide range of pharmacological activities including anti‐HIV , anti‐inflammatory , antibacterial , anticancer , antimalarial agents , as well as α‐glucosidase and acetylcholinesterase inhibitors , and treatment of Alzheimer's disease . Also, coumarins (2 H ‐chromen‐2‐ones) displayed various biological applications such as antifungal, antibacterial, antioxidant, anticoagulant, antiinflammatory, antiviral, anticancer, antitumor, anti‐diabetic, antitubercular, antiplasmodial, and antimalarial activities, as well as fluorescent sensors .…”