Abstract
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.
Keywords: COX-2, Inflammation, PGE2, Cancer, Pain.
Mini-Reviews in Medicinal Chemistry
Title:Desirable Properties for 3rd Generation Cyclooxygenase-2 Inhibitors
Volume: 16 Issue: 16
Author(s): Micky D. Tortorella, Yanmei Zhang and John Talley
Affiliation:
Keywords: COX-2, Inflammation, PGE2, Cancer, Pain.
Abstract: 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.
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Cite this article as:
Tortorella D. Micky, Zhang Yanmei and Talley John, Desirable Properties for 3rd Generation Cyclooxygenase-2 Inhibitors, Mini-Reviews in Medicinal Chemistry 2016; 16 (16) . https://dx.doi.org/10.2174/1389557515666160509125702
DOI https://dx.doi.org/10.2174/1389557515666160509125702 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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