Choi, Ji Won Jang, Bo Ko Cho, Nam-chul Park, Jong-Hyun Yeon, Seul Ki Ju, Eun Ji Lee, Yong Sup Han, Gyoonhee Pae, Ae Nim Kim, Dong Jin Park, Ki Duk 2024-01-20T06:03:09Z 2024-01-20T06:03:09Z 2021-09-04 2015-10 0968-0896 https://pubs.kist.re.kr/handle/201004/124983 We have synthesized three categories of alpha,beta-unsaturated carbonyl derivatives and evaluated their MAO-A and MAO-B inhibitory activities. Among them, compound 10b including alpha, beta-unsaturated ketone group showed the most potent and selective MAO-B inhibitory activity (IC50 human MAO-B 16 nM, >6000-fold selective vs MAO-A) and compound 10b exhibited good reversibility compared with selegiline, a well-known irreversible MAO-B inhibitor. However, both a, b-unsaturated amide and ester derivatives exhibited weaker MAO-B inhibition potencies. The docking studies provided insights into the possible binding modes and the key interaction sites of the synthesized MAO-B inhibitors. (C) 2015 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors Article 10.1016/j.bmc.2015.08.012 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.23, no.19, pp.6486 - 6496 BIOORGANIC & MEDICINAL CHEMISTRY 23 19 6486 6496 N scie scopus 000361638400024 2-s2.0-84942197132 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article PARKINSONS-DISEASE CHALCONE DERIVATIVES B INHIBITORS AMINO-ACID SUBSTRATE UPDATE MODELS POTENT AGENTS alpha,beta-Unsaturated carbonyl derivatives Chalcone Monoamine oxidase MAO-B inhibitor Reversible inhibitor