Synthetic Studies on Analgesic 5-Aminomethylsalicylic Acid

Carboxyarylindoles as nonsteroidal antiinflammatory agents

“…The selection of the substituents examined was such that a relatively wide range of electronic and hydrophobic properties was represented. In several cases (18,20,22,31) the substituted derivatives approached or equaled the potency of the unsubstituted analog 2, but in most cases (19,21,(23)(24)(25)(26)(27)(28)(29) the activity was of a lower order. In general, it appears that for a given substituent (CH3O, for example), activity follows the pattern para > ortho » meta; a Hansch Experimental Section Pharmacology.…”