An Insight into Pyrazole-containing Compounds: Synthesis and Pharmacological Activities

Abstract

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.

Green Synthesis of Pyrazoles: Recent Developments in Aqueous Methods

“…Pyrazole is a versatile ring among heterocyclic compounds as pyrazole compounds are involved in a plethora of applications, including industrial, medical, pharmaceutical, and agricultural uses and as polymers, luminophores, dyes, etc. 15 Pyrazole-containing compounds have various therapeutic and pharmaceutical properties and represent important building blocks for, insecto-acaricidal, antibacterial, antidepressant, analgesic, antiviral, anticancer, antioxidant, anti-HIV, cyclooxygenase-2 (COX-2) inhibitor, anti-inflammatory, antiproliferative drugs. 16 17 18 19 20 21 22 23 24 25 26 Many of the derivatives are of great interest due to their pharmacological properties, for instance, celecoxib {4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide} acts as inhibitor of COX-2 and reduces side effects in the gastrointestinal tract.…”