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Synthesis and biological evaluation of 3-styrylchromone derivatives as selective monoamine oxidase B inhibitors
Get PDFA series of 3-styrylchromone derivatives was synthesized and evaluated for monoamine oxidase (MAO) A and B inhibitory activities. Most of all derivatives inhibited MAO-B selectively, except compound 21. Compound 19, which had a methoxy group at R2 on the chromone ring and chlorine at R4 on phenyl ring, potently inhibited MAO-B, with an IC50 value of 2.2 nM. Compound 1 showed the highest MAO-B selectivity, with a selectivity index of >3700. Further analysis of these compounds indicated that compounds 1 and 19 were reversible and mixed-type MAO-B inhibitors, suggesting that their mode of action may be through tight-binding inhibition to MAO-B.Quantitative structure–activity relationship (QSAR) analyses of the 3-styrylchromone derivatives were conducted using their pIC50 values, through Molecular Operating Environment (MOE) and Dragon. There were 1796 descriptors of MAO-B inhibitory activity, which showed significant correlations (P < 0.05). Further investigation of the 3-styrylchromone structures as useful scaffolds was performed through three-dimensional-QSAR studies using AutoGPA, which is based on the molecular field analysis algorithm using MOE. The MAO-B inhibitory activity model constructed using pIC50 value index exhibited a determination coefficients (R2) of 0.972 and a Leave-One-Out cross-validated determination coefficients (Q2) of 0.914.These data suggest that the 3-styrylchromone derivatives assessed herein may be suitable for the design and development of novel MAO inhibitors.Article No.17506
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Get PDF地域連携報告 / Reports 編集：城西大学・城西短期大学地域連携センター紀要編集委員
Introduction of practical examples of community collaboration and education using J-DAG (Just-Disaster Action Game)
Get PDF地域活動ノート / Notes 編集：城西大学・城西短期大学地域連携センター紀要編集委員
Approach of the Department of Chemistry in Josai University to Kodomo University, Nishi-Iruma
Get PDF 「子ども大学にしいるま」は，城西大学と明海大学・歯学部および坂戸市，毛呂山町，越生町の教育委員会が連携し，坂戸市，毛呂山町，越生町の小学４～６年生を対象にして開催している講座である。子ども大学では，大学教員や地域の専門家から【はてな学】【ふるさと学】【生き方学】の３つの分野を学び，それを通じて子どもの学ぶ力や生きる力を育むことを目的とする。城西大学・理学部化学科では，科学実験を通じて子ども達にものごとの原理や仕組みを追求する力を養ってもらうために【はてな学】を本事業で継続的に開講している。本稿では平成２４年度～令和元年度の化学科の本事業への取り組みについて報告する。実践報告 / Report
