Synthesis and screening of cyclooxygenase inhibitory activity of some 1,3-dioxoisoindoline derivatives

Abstract

In this study, 15 compounds bearing N,N-phthaloylacetamide structure designed by the molecular simplification approach based on thalidomide structure were synthesized and evaluated for inhibitory potencies against cyclooxgenase (COX) isoenzymes, namely COX-1 and COX-2. The results suggested that the N,N-phthaloylacetamide structure, as a primary amide, has inhibitory activity against cyclooxygenase isoenzymes with a higher COX-1 selectivity. The conversion of the primary amide to secondary or tertiary derivatives lowered the potency but favored the COX-2 selectivity thus yielding the compounds with stronger COX-2 inhibiting activity.

Key words

Anti-inflammatories - Cyclooxygenase - 1,3-Dioxoisoindolines, inhibitory activity, synthesis - Thalidomide derivatives

• References

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