Cyclooxygenase (COX) inhibitors: A comparative QSAR study

Cyclooxygenase (COX) or prostaglandin endoperoxide synthase (PGHS) catalyzes the first step in the biosynthesis of the prostaglandins (PGs) from the substrate arachidonic acid (AA). It is established that two distinct COX isoforms exist: the constitutive form (COX-1) expressed virtually in all tissues and the inducible form (COX-2) that is largely restricted to the brain and kidney. Available data showing the association of COX-2 with inflammation led to the hypothesis that selective inhibitors of COX-2 might be inflammatory without the side effects of the current NSAIDS. This paper discusses the QSAR studies on COX-2 inhibitors. It also includes QSAR studies on COX-1 inhibitors for comparison.