Synthesis of some pyridazinylacetic acid derivatives as a novel class of monoamine oxidase-A inhibitors

Sherine Nabil Khattab; Adnan Ahmed Bekhit; Ayman El-Faham; Abdel Moneim El Massry; Adel Amer

doi:10.1248/cpb.56.1717

Synthesis of some pyridazinylacetic acid derivatives as a novel class of monoamine oxidase-A inhibitors

Chem Pharm Bull (Tokyo). 2008 Dec;56(12):1717-21. doi: 10.1248/cpb.56.1717.

Authors

Sherine Nabil Khattab¹, Adnan Ahmed Bekhit, Ayman El-Faham, Abdel Moneim El Massry, Adel Amer

Affiliation

¹ Department of Chemistry, Faculty of Science, University of Alexandria, Alexandria, Egypt.

PMID: 19043245
DOI: 10.1248/cpb.56.1717

Abstract

A series of new pyridazinylacetic acid derivatives were synthesized and have been investigated for their ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO). All compounds were found to be more selective to the MAO-A isoform with compound 5d having the highest SI values. Computational study performed with a docking technique indicated the potential of these compounds in pyridazine-based MAO-A inhibitor drug development.

MeSH terms

Animals
In Vitro Techniques
Indicators and Reagents
Magnetic Resonance Spectroscopy
Mice
Mitochondria, Liver / drug effects
Mitochondria, Liver / enzymology
Models, Molecular
Molecular Conformation
Monoamine Oxidase / metabolism
Monoamine Oxidase Inhibitors / chemical synthesis*
Monoamine Oxidase Inhibitors / pharmacology*
Pyridazines / chemical synthesis*
Pyridazines / pharmacology*
Rats
Serotonin / metabolism
Spectrophotometry, Ultraviolet
Stereoisomerism
Structure-Activity Relationship

Substances

Indicators and Reagents
Monoamine Oxidase Inhibitors
Pyridazines
Serotonin
Monoamine Oxidase