Affiliation:
1. Faculty of Pharmaceutical Sciences, M.M. College of Pharmacy, Maharishi Markandeshwer (Deemed to be
University), Mullana, Ambala, Haryana, India
2. Research Scholar, Institute of Pharmaceutical Sciences, Kurukshetra
University, Kurukshetra, Haryana, India
3. Guru Gobind Singh College of Pharmacy, Yamunanagar, Haryana, India
Abstract
Abstract:
Despite extensive research in the field of drug discovery and development, still there
is a need to develop novel molecular entities. Literature reveals a substantial heterocyclic nucleus
named, piperazine, which shows an immense therapeutic voyage. For several decades, molecules
having the piperazine nucleus have entered the market as a drug exhibiting biological potential. It
was known to possess antipsychotic, antihistamine, antianginal, antidepressant, anticancer, antiviral,
cardioprotective, and anti-inflammatory activity with a specific basis for structural activity
relationship. Thus, it is regarded as a key structural feature in most of the already available therapeutic
drugs in the market. Reports also suggest that the extensive utilization of these currently
available drugs having a piperazine nucleus shows increasing tolerance significantly day by day.
In addition to this, various other factors like solubility, low bioavailability, cost-effectiveness,
and imbalance between pharmacokinetics and pharmacodynamics profile limit their utilization.
Focusing on that issues, various structural modification studies were performed on the piperazine
moiety to develop new derivatives/analogs to overcome the problems associated with available
marketed drugs. Thus, this review article aims to gain insight into the number of structural modifications
at the N-1 and N-4 positions of the piperazine scaffold. This SAR approach may prove
to be the best way to overcome the above-discussed drawbacks and lead to the design of drug
molecules with better efficacy and affinity. Hence, there is an urgent need to focus on the structural
features of this scaffold which paves further work for deeper exploration and may help medicinal
chemists as well as pharmaceutical industries.
Publisher
Bentham Science Publishers Ltd.
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