Background: Due to newly emerging microbial infections and the development of resistance
against cutting-edge therapeutics, innovative and robust medicinal agents are required.
Small ring heterocycles, such as pyrazole and its derivatives have been acknowledged to possess
myriad biological properties and the presence of pyrazole in clinics like celecoxib, phenylbutazone
(anti-inflammatory), CDPPB (antipsychotic), rimonabant (anti-obesity), antipyrine, difenamizole
(analgesic), fipronil (broad-spectrum insecticidal), betazole (H2-receptor agonist) and fezolamide
(antidepressant) drugs has proven the pharmacological perspective of pyrazole nucleus.
Objectives: The current review paper aimed at a recent update made on novel methodologies
adopted in the synthesis of pyrazole derivatives with the emphasis on antibacterial (DNA gyrase
inhibition) and antifungal activities.
Methods: Pyrazole is one of the major tools to be investigated in drug design and discovery. Many
studies have been reported by researchers that have claimed the significant biological potential of
these derivatives. However, numerous studies on pyrazoles compounds shown to exhibit potential
antifungal and antibacterial activities, the focus has also been made on DNA gyrase inhibition.
Additionally, some important patents granted to this heterocyclic nucleus related to antimicrobial
potential are also addressed appropriately.
Results: DNA gyrase is a promising biotarget yet to be explored against a number of medicinal agents.
The present work provides valuable insight into synthetic methods and antibacterials/antifungal significance
of pyrazoles in general as well as new inhibitors of DNA gyrase in particular.
Conclusion: The manuscript constitutes a valuable reference which advocates candidature of pyrazoles
as a potential therapeutic alternative as antibacterial and antifungal agent.