Towards development of selective and reversible pyrazoline based MAO-inhibitors: Synthesis, biological evaluation and docking studies

Anasuya Sahoo; Samiye Yabanoglu; Barij N Sinha; Gulberk Ucar; Arijit Basu; Venkatesan Jayaprakash

doi:10.1016/j.bmcl.2009.11.015

Towards development of selective and reversible pyrazoline based MAO-inhibitors: Synthesis, biological evaluation and docking studies

Bioorg Med Chem Lett. 2010 Jan 1;20(1):132-6. doi: 10.1016/j.bmcl.2009.11.015. Epub 2009 Nov 12.

Authors

Anasuya Sahoo¹, Samiye Yabanoglu, Barij N Sinha, Gulberk Ucar, Arijit Basu, Venkatesan Jayaprakash

Affiliation

¹ Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835 215, India.

PMID: 19945874
DOI: 10.1016/j.bmcl.2009.11.015

Abstract

Ten novel 3,5-diaryl pyrazolines were synthesized and investigated for their monoamine oxidase (MAO) inhibitory property. All the molecules were found to be reversible and selective inhibitor for either one of the isoform (MAO-A or MAO-B). Further insights in the theoretical evaluation of the possible interactions between the compounds and monoamine oxidases (MAO-A or MAO-B) have been developed through docking studies. The theoretical values are in congruence with their experimental values.

MeSH terms

Animals
Binding Sites
Computer Simulation
Humans
Hydrogen Bonding
Liver / enzymology
Monoamine Oxidase / chemistry*
Monoamine Oxidase / metabolism
Monoamine Oxidase Inhibitors / chemical synthesis*
Monoamine Oxidase Inhibitors / chemistry
Monoamine Oxidase Inhibitors / pharmacology
Protein Isoforms / chemistry
Protein Isoforms / metabolism
Pyrazoles / chemical synthesis*
Pyrazoles / chemistry
Pyrazoles / pharmacology
Rats
Sulfonamides / chemical synthesis*
Sulfonamides / chemistry
Sulfonamides / pharmacology

Substances

Monoamine Oxidase Inhibitors
Protein Isoforms
Pyrazoles
Sulfonamides
Monoamine Oxidase