Novel monoamine oxidase inhibitors based on the privileged 2-imidazoline molecular framework.

Dose-Response Relationship, Drug Humans Imidazoles / chemical synthesis Molecular Structure Monoamine Oxidase / metabolism Monoamine Oxidase Inhibitors / chemical synthesis Neurodegenerative Diseases / drug therapy Structure-Activity Relationship
2-Imidazoline Inhibition MAO Monoamine oxidase Selective

Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
01 01 2019
Historique:
received: 17 09 2018
revised: 06 11 2018
accepted: 08 11 2018
pubmed: 21 11 2018
medline: 5 11 2019
entrez: 21 11 2018
Statut: ppublish

Résumé

Series of structurally diverse 2-imidazoline derivatives have been synthesized by condensation of substituted aldehydes with ethylenediamine, Pd-catalyzed N-arylation of 2-imidazolines and by the formation of 1,2,4-oxadiazoles and benzoxazepines from 2-imidazoline-containing precursors. The 2-imidazoline derivatives were evaluated as potential inhibitors of human monoamine oxidase (MAO) A and B. Among the 2-imidazolines, good potency inhibitors were discovered with compound 9p (IC

Identifiants

DOI: 10.1016/j.bmcl.2018.11.018 PMID: 30455149
pubmed: 30455149
pii: S0960-894X(18)30883-7
doi: 10.1016/j.bmcl.2018.11.018
pii:
doi:

Substances chimiques

Imidazoles 0
Monoamine Oxidase Inhibitors 0
2-imidazoline D36R5YLK6R
Monoamine Oxidase EC 1.4.3.4
monoamine oxidase A, human EC 1.4.3.4.

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

40-46

Informations de copyright

Copyright © 2018 Elsevier Ltd. All rights reserved.

Auteurs

Anton Shetnev (A)

Pharmaceutical Technology Transfer Center, Ushinsky Yaroslavl State Pedagogical University, 108 Respublikanskaya St., Yaroslavl 150000, Russian Federation. Electronic address: a.shetnev@yspu.org.

Angelina Osipyan (A)

Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii Prospect, Peterhof, Saint Petersburg 198504, Russian Federation. Electronic address: angelina.osipyan@gmail.com.

Sergey Baykov (S)

Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii Prospect, Peterhof, Saint Petersburg 198504, Russian Federation. Electronic address: sergei.v.baikov@yandex.ru.

Alexander Sapegin (A)

Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii Prospect, Peterhof, Saint Petersburg 198504, Russian Federation. Electronic address: sapegin_yar@mail.ru.

Zhanna Chirkova (Z)

Yaroslavl State Technical University, 150023 Yaroslavl, Russian Federation. Electronic address: chirkovazhv@ystu.ru.

Michail Korsakov (M)

Pharmaceutical Technology Transfer Center, Ushinsky Yaroslavl State Pedagogical University, 108 Respublikanskaya St., Yaroslavl 150000, Russian Federation. Electronic address: mkkors@mail.ru.

Anél Petzer (A)

Pharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa. Electronic address: 12264954@nwu.ac.za.

Idalet Engelbrecht (I)

Pharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa. Electronic address: idalet.engelbrecht@gmail.com.

Jacobus P Petzer (JP)

Pharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa. Electronic address: jacques.petzer@nwu.ac.za.

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Classifications MeSH

questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Novel monoamine oxidase inhibitors based on...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Novel monoamine oxidase inhibitors based on...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Imidazoles › Novel monoamine oxidase inhibitors based on...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Novel monoamine oxidase inhibitors based on...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Oxidoreductases acting on CH-NH2 group donors › Monoamine oxidase › Novel monoamine oxidase inhibitors based on...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de la monoamine oxydase › Novel monoamine oxidase inhibitors based on...
questionsmedicales.fr › Maladies du système nerveux › Maladies neurodégénératives › Novel monoamine oxidase inhibitors based on...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Novel monoamine oxidase inhibitors based on...