Non-steroidal anti-inflammatory drugs: recent advances in the use of synthetic COX-2 inhibitors

Abstract

Overview of the structure and function of recent synthetic COX-2 inhibitors and the mechanism of action inside the active-site cavity.

Development of Novel 1,3-Disubstituted-2-Thiohydantoin Analogues with Potent Anti-Inflammatory Activity; In Vitro and In Silico Assessments

“…While COX-1 is expressed in several tissues, the expression of COX-2 is mainly overexpressed in various cell types by several inducers including hormones, growth factors, cytokines, and lipopolysaccharide [ 81 , 82 , 83 , 84 , 85 ]. Several studies have indicated that the required anti-inflammatory, antipyretic and analgesic activities of NSAID are mainly due to the inhibition of COX-2 activity, whereas the adverse effects of these drugs is assigned to the inactivation of COX-1 activity [ 86 , 87 , 88 ]. Furthermore, it has been shown that COX-2 is overexpressed in several neurodegenerative diseases, angiogenesis, and cancer [ 89 , 90 , 91 , 92 ].…”

The indole nucleus as a selective COX-2 inhibitor and anti-inflammatory agent (2011–2022)

“…36 The mechanism of inflammation is initiated via the phospholipase enzyme which is responsible for the conversion of phospholipids present in the cell membrane into arachidonic acid which is further catalysed by cyclooxygenase and lipoxygenase enzymes to furnish prostaglandins and leukotrienes respectively. [37][38][39] Prostaglandins are responsible for many inflammatory diseases such as asthma, arthritis and skin inflammation where they mediate the inflammatory action of the platelet activation factors (PAFs). 40,41 The pharmacological inhibition of COX enzymes has been found to be useful in getting relief from pain and inflammation.…”

Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses

“…The chosen moiety on the other side of the ester linkage was preferably to be another active agent to achieve dual-target activity. NSAIDs are analgesic, antipyretic and anti-inflammatory medications, widely used to relieve symptoms related to many conditions, including viral colds [ 18 ]. Side effects, particularly gastrointestinal ulcerogenic activity and renal toxicity, often limit their use.…”