MAO Inhibitory Activity of 4, 5-Dihydro-1 HPyrazole Derivatives: A Platform To Design Novel Antidepressants
Pp. 47-91 (45)
Vishnu Nayak Badavath and Venkatesan Jayaprakash
Emergence of treatment-resistant depression is the new challenge before us.
As antidepressants currently existing in the market are of little or no use, clinicians are
looking for newer and effective antidepressants to handle situations. Inhibition of
Monoamine oxidase, an effective strategy discontinued a few decades before due to
selectivity related issues. Technological advancement in chemistry and biology
interface is now availing hopes of achieving the design and synthesis of novel,
isoform-selective and tissue-specific inhibitors. This has renewed the interest in reexploring
the MAO inhibitors in the past decade. Under this background, the chapter
reviews MAO inhibitory activity and antidepressant activity of 4, 5-dihydro-1Hpyrazole
derivatives reported to date. Since different sources of enzymes (rat, bovine,
human, etc.) were used by different groups to evaluate the newly synthesized
compounds, any discussion on structure-activity-relationship may not be justified.
Hence, the authors made an attempt to summarize the literature based on the chemical
architecture of the compounds that may help the medicinal chemists to further explore
the unexplored chemical space. Further, efforts by the scientific community to report
the effect of chirality of compounds on activity and selectivity, experimentally or
through computational simulations are also documented.
4, 5-Dihydro-1H-Pyrazole Derivatives, Antidepressant Activity,
Chiral Separation and Computational Studies, MAO Inhibitory Activity.
Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology-Mesra, Ranchi-835215, Jharkhand, India.