ANTIINFLAMMATORY 4,5-DIARYLPYRROLES - SYNTHESIS AND QSAR

A series of 2-substituted- and rophenyl)-5-[4-(methylsulfonyl)phenyl]- 1H-pyrroles was synthesized and found to be active in the rat adjuvant arthritis model of inflammation. The most active compounds were the 2 -halo derivatives in the order of chloro > bromo > iodo. The same patt ern of activity was observed for the 2,3-dihalopyrroles. Quantitative structure-activity relationship studies suggested that the activity co uld be correlated with the molar refractivity and the inductive field effect of the 2-substituent and the lipophilicity of the 3-substituent .