FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W69154181> ?p ?o ?g. }

• W69154181 endingPage "451" @default.
• W69154181 startingPage "441" @default.
• W69154181 abstract "Monoamine oxidase (MAO) assay specificity based on substrate specificity was investigated by substrate competition experiments. 10 μM serotonin (5-HT) and 5 μM β-phenylethylamine (PEA) were found to ensure total substrate specificity for, respectively, MAO types A and B. Twenty-five 2-aryl-4H-1,3,4-oxadiazin-5(6H)-one derivatives were synthesized and tested in vitro for their inhibitory effects on MAO A and B. Most of them inhibited preferentially MAO B. The 2-(4-biphenylyl)-4-(2-cyanoethyl)-4H-1,3,4-oxadiazin-5(6H)-one 32 was the most efficient MAO B inhibitor and acted as a competitive inhibitor on the two enzymes. Its Ki values for MAO A and B were 11 and 0.15 μM, respectively. Structure-activity relationships suggest that these oxadiazinones should interact with a hydrophobic site and a nucleophilic site on MAO B for binding, while the functional group of the N-4 substituent should compete with the substrate for the active site of the enzyme. La spécificité du dosage de la monoamine oxydase (MAO) a étéétudiée par des expériences de compétition. Les concentrations de 10 μM pour la 5-HT et de 5 μM pour la PEA assurent une spécificité totale du dosage respectivement pour les MAO A et B. Vingt cinq dérivés d'aryl-2 4H-oxadiazine-1,3,4 (6H) ones-5 ont été synthétisés et testés in vitro pour leur activité inhibitrice sur les MAO A et B. La plupart de ces composés inhibent préférentiellement la MAO B. La (biphénylyl-4)-2 (cyano-2 éthyl)-4 4H-oxadiazine-1,3,4 (6H)one-5 32 est l'inhibiteur le plus efficace de la série sur la MAO B et agit de façon compétitive sur les deux types d'enzyme. Les valeurs des Ki pour ce composé 32 vis-à-vis des MAO A et B sont égales respectivement à 11 et 0,15 μM. Les relations structure-activité suggèrent que des interactions avec un site hydrophobe et un site nucléophile de la MAO B interviendraient dans la fixation de l'inhibiteur alors que le groupe fonctionnel du substituant en position 4 entrerait en compétition avec le substrat pour le site actif de l'enzyme." @default.
• W69154181 created "2016-06-24" @default.
• W69154181 creator A5029787028 @default.
• W69154181 creator A5047542019 @default.
• W69154181 creator A5047733350 @default.
• W69154181 creator A5084852513 @default.
• W69154181 date "1988-10-01" @default.
• W69154181 modified "2023-10-06" @default.
• W69154181 title "Inhibition des monoamine oxydases A et B par des dérivés d'aryl-2 4H-oxadiazine-1,3,4 (6H) ones-5" @default.
• W69154181 cites W152815861 @default.
• W69154181 cites W1598486575 @default.
• W69154181 cites W1968257988 @default.
• W69154181 cites W1976572110 @default.
• W69154181 cites W1982072964 @default.
• W69154181 cites W1996755503 @default.
• W69154181 cites W2000817354 @default.
• W69154181 cites W2018990600 @default.
• W69154181 cites W2019883162 @default.
• W69154181 cites W2029800949 @default.
• W69154181 cites W2034604257 @default.
• W69154181 cites W2043254626 @default.
• W69154181 cites W2051254875 @default.
• W69154181 cites W2057864290 @default.
• W69154181 cites W2074470137 @default.
• W69154181 cites W2075191327 @default.
• W69154181 cites W2077245981 @default.
• W69154181 cites W2083612512 @default.
• W69154181 cites W2090114150 @default.
• W69154181 cites W2119281073 @default.
• W69154181 cites W2143857681 @default.
• W69154181 cites W2262635949 @default.
• W69154181 cites W2266631600 @default.
• W69154181 cites W2336388410 @default.
• W69154181 cites W2409295204 @default.
• W69154181 cites W2409489881 @default.
• W69154181 cites W2474635282 @default.
• W69154181 doi "https://doi.org/10.1016/0223-5234(88)90141-9" @default.
• W69154181 hasPublicationYear "1988" @default.
• W69154181 type Work @default.
• W69154181 sameAs 69154181 @default.
• W69154181 citedByCount "29" @default.
• W69154181 countsByYear W691541812015 @default.
• W69154181 countsByYear W691541812017 @default.
• W69154181 countsByYear W691541812018 @default.
• W69154181 crossrefType "journal-article" @default.
• W69154181 hasAuthorship W69154181A5029787028 @default.
• W69154181 hasAuthorship W69154181A5047542019 @default.
• W69154181 hasAuthorship W69154181A5047733350 @default.
• W69154181 hasAuthorship W69154181A5084852513 @default.
• W69154181 hasConcept C153911025 @default.
• W69154181 hasConcept C170493617 @default.
• W69154181 hasConcept C178790620 @default.
• W69154181 hasConcept C181199279 @default.
• W69154181 hasConcept C185592680 @default.
• W69154181 hasConcept C187714386 @default.
• W69154181 hasConcept C2775864247 @default.
• W69154181 hasConcept C2776024655 @default.
• W69154181 hasConcept C2780263894 @default.
• W69154181 hasConcept C2781076698 @default.
• W69154181 hasConcept C39398028 @default.
• W69154181 hasConcept C55493867 @default.
• W69154181 hasConcept C71240020 @default.
• W69154181 hasConcept C86803240 @default.
• W69154181 hasConceptScore W69154181C153911025 @default.
• W69154181 hasConceptScore W69154181C170493617 @default.
• W69154181 hasConceptScore W69154181C178790620 @default.
• W69154181 hasConceptScore W69154181C181199279 @default.
• W69154181 hasConceptScore W69154181C185592680 @default.
• W69154181 hasConceptScore W69154181C187714386 @default.
• W69154181 hasConceptScore W69154181C2775864247 @default.
• W69154181 hasConceptScore W69154181C2776024655 @default.
• W69154181 hasConceptScore W69154181C2780263894 @default.
• W69154181 hasConceptScore W69154181C2781076698 @default.
• W69154181 hasConceptScore W69154181C39398028 @default.
• W69154181 hasConceptScore W69154181C55493867 @default.
• W69154181 hasConceptScore W69154181C71240020 @default.
• W69154181 hasConceptScore W69154181C86803240 @default.
• W69154181 hasIssue "5" @default.
• W69154181 hasLocation W691541811 @default.
• W69154181 hasOpenAccess W69154181 @default.
• W69154181 hasPrimaryLocation W691541811 @default.
• W69154181 hasRelatedWork W1967398722 @default.
• W69154181 hasRelatedWork W1996784854 @default.
• W69154181 hasRelatedWork W2005665072 @default.
• W69154181 hasRelatedWork W2041489176 @default.
• W69154181 hasRelatedWork W2071330786 @default.
• W69154181 hasRelatedWork W2247799850 @default.
• W69154181 hasRelatedWork W2307491850 @default.
• W69154181 hasRelatedWork W2322941916 @default.
• W69154181 hasRelatedWork W2395399931 @default.
• W69154181 hasRelatedWork W4246748827 @default.
• W69154181 hasVolume "23" @default.
• W69154181 isParatext "false" @default.
• W69154181 isRetracted "false" @default.
• W69154181 magId "69154181" @default.
• W69154181 workType "article" @default.