Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase.

Acetylcholinesterase / chemistry Alkynes / chemical synthesis Alzheimer Disease / drug therapy Catalytic Domain Cell Line, Tumor Cholinesterase Inhibitors / chemical synthesis Drug Design Humans Kinetics Molecular Docking Simulation Molecular Dynamics Simulation Molecular Structure Monoamine Oxidase / chemistry Monoamine Oxidase Inhibitors / chemical synthesis Pyrimidines / chemical synthesis Structure-Activity Relationship
Acetylcholinesterase inhibitors Alzheimer's disease Diphenylpyrimidine Dual inhibitors MAO inhibitors Neurological disorders

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
01 Sep 2019
Historique:
received: 05 02 2019
revised: 24 04 2019
accepted: 13 05 2019
pubmed: 1 6 2019
medline: 26 7 2019
entrez: 1 6 2019
Statut: ppublish

Résumé

Alzheimer's disease (AD) is a multifactorial neurological disorder involving complex pathogenesis. Single target directed drugs proved ineffective and since last few years' different pharmacological strategies including multi-targeting agents are being explored for the effective drug development for AD. A total of 19 dipropargyl substituted diphenylpyrimidines have been synthesized and evaluated for the monoamine oxidase (MAO) and acetylcholinesterase (AChE) inhibition potential. All the compounds were found to be selective and reversible inhibitors of MAO-B isoform. These compounds also displayed good AChE inhibition potential with IC

Identifiants

DOI: 10.1016/j.ejmech.2019.05.039 PMID: 31151057
pubmed: 31151057
pii: S0223-5234(19)30449-0
doi: 10.1016/j.ejmech.2019.05.039
pii:
doi:

Substances chimiques

Alkynes 0
Cholinesterase Inhibitors 0
Monoamine Oxidase Inhibitors 0
Pyrimidines 0
Monoamine Oxidase EC 1.4.3.4
Acetylcholinesterase EC 3.1.1.7

Types de publication

Journal Article

Langues

eng

Pagination

221-234

Informations de copyright

Copyright © 2019. Published by Elsevier Masson SAS.

Auteurs

Bhupinder Kumar (B)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab, 151001, India.

Vijay Kumar (V)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab, 151001, India.

Vikash Prashar (V)

Department of Animal Sciences, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, Punjab, India.

Suresh Saini (S)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab, 151001, India.

Ashish Ranjan Dwivedi (AR)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab, 151001, India.

Beenu Bajaj (B)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab, 151001, India.

Devashish Mehta (D)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab, 151001, India.

Jyoti Parkash (J)

Department of Animal Sciences, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, Punjab, India. Electronic address: Jyoti.parkash@cup.edu.in.

Vinod Kumar (V)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab, 151001, India. Electronic address: vpathania18@gmail.com.

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Classifications MeSH

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Carboxylic ester hydrolases › Cholinesterases › Acetylcholinesterase › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures acycliques › Alcynes › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Conformation moléculaire › Conformation des protéines › Éléments structuraux des protéines › Domaine catalytique › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Anticholinestérasiques › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Cinétique › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de dynamique moléculaire › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Oxidoreductases acting on CH-NH2 group donors › Monoamine oxidase › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de la monoamine oxydase › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrimidines › Dipropargyl substituted diphenylpyrimidines as...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Dipropargyl substituted diphenylpyrimidines as...