Arzneimittelforschung, Table of Contents Arzneimittelforschung 2011; 61(3): 186-190DOI: 10.1055/s-0031-1296187 Analgesics · Anti-inflammatories · Antiphlogistics · Antirheumatic Drugs Editio Cantor Verlag Aulendorf (Germany)Synthesis and screening of cyclooxygenase inhibitory activity of some 1,3-dioxoisoindoline derivatives Authors Author Affiliations Murat Çizmecioğlu 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University Bornova, Izmir, Turkey Varol Pabuççuoğlu 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University Bornova, Izmir, Turkey Petek Ballar 2 Department of Biochemistry, Faculty of Pharmacy, Ege University Bornova, Izmir, Turkey Aysun Pabuççuoğlu 2 Department of Biochemistry, Faculty of Pharmacy, Ege University Bornova, Izmir, Turkey Zeynep Soyer 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University Bornova, Izmir, Turkey Recommend Article Abstract Buy Article(opens in new window) 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 Key wordsAnti-inflammatories - Cyclooxygenase - 1,3-Dioxoisoindolines, inhibitory activity, synthesis - Thalidomide derivatives Full Text References References 1 Aggarwal BB, Shishodia S, Sandur SK, Pandey MK, Sethi G. Inflammation and cancer: How hot is the link?. Biochem Pharmacol. 2006; 72: 1605-21 2 Pelletier JM, Lajeunesse D, Reboul P, Pelletier JP. Therapeutic role of dual inhibitors of 5-LOX and COX, selective and non-selective non-steroidal anti-inflammatory drugs. Ann Rheum Dis. 2003; 62: 501-9 3 Rao PNP, Knaus EE. 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