Aspirin (II) Structure-Activity Relationship of Salicylates and Improvements of Their Therapeutic Value through Structural Modification

Since the introduction of aspirin as a therapeutic agent in 1899, there have been numerous attempts at the improvement of its therapeutic value through molecular modification. These endeavors have centered mainly around the following two approaches : (a) improvement of the potency by introduction of a suitable group or groups on the benzene ring; and (b) modification of the carboxylic acid group, which is thought to be an immediate cause of the irritant effect.