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

Cizmecioglu M., Pabuccuoglu V., Ballar P. , Pabuccuoglu A., SOYER Z.

ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, cilt.61, ss.186-190, 2011 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 61 Konu: 3
  • Basım Tarihi: 2011
  • Sayfa Sayıları: ss.186-190


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.