Structural Insights into Pyrazoles as Agents against Anti‐inflammatory and Related Disorders

Abstract

Pyrazole moiety is considered as the most important therapeutic agent for the treatment of inflammation and inflammation associated cancers. Celecoxib, Ramifenazone, Rimonabant and Lonazolac are some of the commercially available pyrazole moieties which are potent COX‐2 inhibitors and also acts in inhibiting various cancers. Recently there are numerous reviews on the biological significance of pyrazole derivatives. However, this review discusses pyrazole derivatives possessing anti‐inflammatory and anticancer activity (COX inhibition) and also illustrates the recent updates on pyrazole research emphasizing on the medicinal chemistry aspects such as the key structural fragments required for the biological activity. There are series of pyrazoles like di‐substituted, tri‐substituted, tetra‐substituted pyrazoles, pyrazole hydrazones, pyrazoles bearing various other heterocycles, bicyclic fused pyrazoles, tricyclic fused pyrazoles, and miscellaneous class of pyrazoles. All these pyrazoles are being researched as COX inhibitors, anti‐inflammatory and against related disorders like cancer.

Novel Regioselective Synthesis of 1,3,4,5-Tetrasubstituted Pyrazoles and Biochemical Valuation on F1FO-ATPase and Mitochondrial Permeability Transition Pore Formation

“…Among others, Pzs present significant antibacterial [ 11 ], antimicrobic, anticancer, anti-inflammatory, anti-diabetic, and anti-degenerative activity [ 12 ]. In Figure 1 , Betazole [ 13 ], CDPPB [ 14 ], Difenamizole [ 15 ], Fezolamine [ 16 ], Rimonabant [ 17 ], and Ruxolitinib [ 18 , 19 ] are examples of Pz-containing drugs already available on the market ( Figure 1 ).…”

Development and Antibacterial Properties of 4-[4-(Anilinomethyl)-3-phenylpyrazol-1-yl]benzoic Acid Derivatives as Fatty Acid Biosynthesis Inhibitors

“…Pyrazole derivatives are known for their wide range of therapeutic properties. − Three of the 17 small molecule drugs approved in 2022 contain the pyrazole nucleus . Several drugs containing pyrazole moiety have been approved recently, and this nucleus was rare in drugs approved before 2016.…”

Photoinduced 1,3‐Dipolar Cycloadditions of Cyclic Enones and 2,5‐Disubstituted Tetrazoles: An Unprecedented Pathway to Polysubstituted Pyrazolines and Pyrazoles

“…The design and synthesis of nitrogen-containing heterocyclic compounds are of increasing interest because of their wide applications in the pharmaceutical and agrochemical industries. [1] Among them, derivatives of pyrazoline and pyrazole (Figure 1) which are widely studied for their therapeutic potentials, including anticancer, [2] antiinflammatory, [3] and antimicrobial activities [4] among others, [5][6][7][8][9][10][11][12] occupy a prominent place.…”