Chirattikan MaicheenJiraporn Ungwitayatornจิรภรณ์ อังวิทยาธรMahidol University. Faculty of Pharmacy. Department of Pharmaceutical ChemistryHuachiew Chalermprakiet. Faculty of Pharmaceutical Science2020-01-272020-01-272020-01-272019https://repository.li.mahidol.ac.th/handle/20.500.14594/49689The 1st Pharmaceutical Sciences Asia Conference 2019 Theme : Pharmaceutical Sciences toward Health Innovation in the Disruptive Era. Bangkok Midtown Hotel, Thailand. August 22, 2019, page 30A series of chromone derivatives were evaluated as antimalarial and β-hematin formation inhibitory activities. The in vitro antimalarial activity was evaluated using the microculture radioisotope assay. The three most potent antimalarial compounds were 34, 36 and 39 with IC50 = 3.82, 0.95 and 4.87 μM, respectively. Compound 36, the most active, showed higher potency than primaquine and tafenoquine. For β-hematin formation inhibitory activity assay, the top six most potent compounds, 23-28 (IC50 = 1.41, 1.76, 2.30, 2.54, 4.60 and 3.69 μM, respectively) were more potent than chloroquine, dihydroartemisinin, and mefloquine. The ability of chromone compounds to interact and form complex with heme was investigated by the continuous variation technique (Job’s plot). Compounds 28, 38 and 42 interacted with heme with stoichiometric ratio of chromone:heme = 1:1, same ratio as dihydroartemisinin. Compounds 3, 4, 23, 24, 27 and 43 showed the stoichiometric ratio = 1:2, same as chloroquine and mefloquine and compound 36 showed stoichiometric ratio = 1:3.engMahidol Universityantimalarial activityβ-hematin formation inhibitory activitychromone derivativesmicroculture radioisotope assayProceeding AbstractFaculty of Pharmacy Mahidol University