Desirable Properties for 3rd Generation Cyclooxygenase-2 Inhibitors

• Published in: Mini reviews in medicinal chemistry Vol. 16; no. 16; p. 1284
• Main Authors: Tortorella, Micky D, Zhang, Yanmei, Talley, John
• Format: Journal Article
• Language: English
• Published: Netherlands 01.01.2016
• Subjects: Cyclooxygenase 2 - metabolism; Cyclooxygenase 2 Inhibitors - chemistry; Cyclooxygenase 2 Inhibitors - pharmacology; Humans
• ISSN: 1875-5607
• DOI: 10.2174/1389557515666160509125702

Coxibs are a class of powerful drugs used by millions of people worldwide to treat a wide variety of ailments such as muscular skeletal pain and inflammation. The primary mechanism of action of coxibs is the potent inhibition of the COX-2 enzyme. Unfortunately, their use is limited to patients due to a variety of factors including poor solubility, negative effects on renal clearance and increased risk of cardiovascular pathology. However, because of their effectiveness in blocking PGE2 mediated inflammation, a key pathway that drives many diseases, there is a clear unmet medical need to develop new COX-2 inhibitors that are free of the aforementioned problems. The purpose of this prospectus is to define the specific properties that are desired in 3rd generation coxibs as a starting point for the development of new and better drugs.