Chromenylchalcones with inhibitory effects on monoamine oxidase B
- Chromenylchalcones with inhibitory effects on monoamine oxidase B
- 조근형; 안승현; 김봉규; 박혜리; 김영화; 추현아; 고동수; 정유훈; 안중훈; 임융호
- MOA-B; monoamine oxidase; Chromenylchalcone; molecular modeling; SAR; Flavonoid; In silico docking; Monoamine oxidase B
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 21, NO 24, 7890-7897
- Structure–activity relationship (SAR) calculations were used to find monoamine oxidase-B (MAO-B) inhibitors by identifying pharmacophores exhibiting high inhibitory activities. Several such chromenylchalcones were designed and synthesized accordingly. Their inhibitory effects on MAO-B were determined using an HPLC-based method and an MAO-B enzyme assay kit. (E)-3-(6-Methoxy-2H-chromen-3-yl)-1-(2-methoxyphenyl)prop-2-en-1-one exhibited a half-maximal inhibitory concentration of 320 nM. Its molecular-level binding mode with the three-dimensional structure of MAO-B was elucidated using an in silico docking study. The chromenylchalcone scaffold, which is derived from natural products including isoflavonoids and chalcones, had not been previously reported as an MAO-B inhibitor
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