Frontiers in Drug Design and Discovery

Frontiers in Drug Design and Discovery

Volume: 10

Frontiers in Drug Design and Discovery is a book series devoted to publishing the latest and the most important advances in drug design and discovery. Eminent scientists have contributed chapters ...
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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.