Depression is one of the key conditions addressed by the Mental Health Gap Action
Programme (mhGAP) of WHO that can lead to self-harm and suicide. Depression is associated
with low levels of neurotransmitters, which eventually play a key role in the progression and development
of mental illness. The nitrogen-containing heterocyclic compounds exhibit the most
prominent pharmacological profile as antidepressants. Pyrazoline, a dihydro derivative of pyrazole,
is a well-known five-membered heterocyclic moiety that exhibits a broad spectrum of biological
activities. Many researchers have reported pyrazoline scaffold-containing molecules as
potential antidepressant agents with selectivity for monoamine oxidase enzyme (MAO) isoforms.
Several studies indicated a better affinity of pyrazoline-based moiety as (monoamine oxidase inhibitors)
MAOIs. In this review, we have focused on the recent advancements (2019-2023) in the
development of pyrazoline-containing derivatives exhibiting promising inhibition of MAO-A enzyme
to treat depression. This review provides structural insights on pyrazoline-based molecules
along with their SAR analysis, in silico exploration of binding interactions between pyrazoline
derivatives and MAO-A enzyme, and clinical trial status of various drug molecules against depression.
The in-silico exploration of potent pyrazoline derivatives at the active site of the MAOA
enzyme will provide further insights into the development of new potential MAO-A inhibitors
for the treatment of depression.