Background: Newly emerging microbial infections and development of resistance against cutting-edge therapeutics has created deep necessity for innovative and robust medicinal agents. Small ring heterocycles, such as pyrazole and its derivatives have been acknowledged to possess myriad biological properties and 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 have proven the pharmacological perspective of pyrazole nucleus. Objectives: The current review paper aimed at recent update made on novel methodologies adopted in synthesis of pyrazole derivatives with emphasis on antibacterial (DNA gyrase inhibition) and antifungal activities. Method: Pyrazole is one of the major tools to be investigated in drug design and discovery. Many studies have been reported by researchers that has 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, the some important patents granted to this heterocyclic nucleus related to antimicrobial potential are also addressed appropriately. Results: DNA gyrase is 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.

Background: Heterocyclic scaffolds have gained exceptional devotion in the recent years due to their marked utility in bio-organic field. Among these, pyrazole remains a privileged scaffold as broad array of medicinally active agents encompasses this heterocycle as a core nucleus. Pyrazole is a five-membered, aromatic ring containing two nitrogen atoms at adjacent positions are readily able to show interactions with numerous receptor (s), enzymes located on the target cells in biological system. Pyrazole-containing compounds are acknowledged with anticyclooxygenases (anti-inflammatory), carbonic anhydrase inhibitor, α-glycosidase inhibitor, and cholinesterase enzymes inhibitor and anti-DNA gyrases activities. Noticeably, rimonabant, phenylbutazone, fipronil, difenamizole, celecoxib, antipyrine, fezolamide and betazole are few representatives of pyrazole containing drugs. Objectives: The manuscript aims to review the detailed synthetic approaches applied for the synthesis of pyrazole derivatives. In particular, we examine recent scientific finding on antimicrobial, anti-tubercular, antiviral, anticancer and anti-inflammatory perspectives of pyrazole containing analogues. Methods: Pyrazole analogues have been widely explored by scientific community as large number of papers has been published in this regard. Numerous pyrazole-containing analogues have been designed, synthesized, and screened for their in vitro and in vivo bio-efficacy and many of them endowed with commendable pharmacological activities. Pyrazole analogues with superior applications as antiviral, anticancer, and anti-inflammatory efficacy have also been well documented in patents granted to this heterocyclic nucleus. Results: This review outlines the recent advances in medicinal chemistry of pyrazole analogues with a special emphasize of structure-activity relationships to afford ideas for the rational drug-design and discovery and their impact on desired pharmacological applications. Conclusion: The information provided in this manuscript may help the medicinal chemists to generate robust pyrazole analogues with high efficacy.