4,6-Diphenylpyrimidine Derivatives as Dual Inhibitors of Monoamine Oxidase and Acetylcholinesterase for the Treatment of Alzheimer's Disease.

Acetylcholinesterase / metabolism Alzheimer Disease / drug therapy Cell Line, Tumor Cholinesterase Inhibitors / chemical synthesis Humans Monoamine Oxidase / metabolism Monoamine Oxidase Inhibitors / chemical synthesis Pyrimidines / chemical synthesis Structure-Activity Relationship
Alzheimer’s disease MAO inhibitors acetylcholinesterase inhibitors diphenylpyrimidine dual inhibitors neuroprotective agents

Journal

ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337

Informations de publication

Date de publication:
16 01 2019
Historique:
pubmed: 9 10 2018
medline: 7 2 2020
entrez: 9 10 2018
Statut: ppublish

Résumé

Alzheimer's disease (AD) is a neurodegenerative disorder with multifactorial pathogenesis. Monoamine oxidase (MAO) and acetylcholinesterase enzymes (AChE) are potential targets for the treatment of AD. A total of 15 new propargyl containing 4,6-diphenylpyrimidine derivatives were synthesized and screened for the MAO and AChE inhibition activities along with ROS production inhibition and metal-chelation potential. All the synthesized compounds were found to be selective and potent inhibitors of MAO-A and AChE enzymes at nanomolar concentrations. VB1 was found to be the most potent MAO-A and BuChE inhibitor with IC

Identifiants

DOI: 10.1021/acschemneuro.8b00220 PMID: 30296051
pubmed: 30296051
doi: 10.1021/acschemneuro.8b00220
doi:

Substances chimiques

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

252-265

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.

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.

Bibekananda Sarkar (B)

Department of Animal Sciences, School of Basic and Applied Sciences , Central University of Punjab , Bathinda , Punjab 151001 , India.

Sukesh Kumar Gupta (SK)

Department of Pharmaceutical Engineering and Technology , Indian Institute of Technology (Banaras Hindu University) , Varanasi 221005 , India.

Sairam Krishnamurthy (S)

Department of Pharmaceutical Engineering and Technology , Indian Institute of Technology (Banaras Hindu University) , Varanasi 221005 , India.

Anil K Mantha (AK)

Department of Animal Sciences, School of Basic and Applied Sciences , 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 151001 , India.

Vinod Kumar (V)

Laboratory of Organic and Medicinal Chemistry, Department of Pharmaceutical Sciences and Natural Products , Central University of Punjab , Bathinda , Punjab 151001 , India.
ORCID: 0000-0002-1438-9438

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Classifications MeSH

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Carboxylic ester hydrolases › Cholinesterases › Acetylcholinesterase › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Anticholinestérasiques › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Oxidoreductases acting on CH-NH2 group donors › Monoamine oxidase › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de la monoamine oxydase › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrimidines › 4,6-Diphenylpyrimidine Derivatives as Dual...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › 4,6-Diphenylpyrimidine Derivatives as Dual...