Synthesis and screening of cyclooxygenase inhibitory activity of some 1,3-dioxoisoindoline derivatives
Makaleler > Tam Makale · 2011
Yazarlar: Murat Cizmecioglu, Mehmet Varol PABUÇÇUOĞLU, Petek BALLAR KIRMIZIBAYRAK, Nefise Aysun PABUÇÇUOĞLU, Zeynep SOYER
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH, SCI Expanded İndekslerine Giren Dergi, Uluslararası, 2011, cilt 61, ss 186-190
Özet
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.