새로운 계열의 선택적 COX-2 저해제: Lutonin A 동족체 및 그 질소 유도체

A New Class of S elective COX-2 Inhibitor: Luotonin A Homoligues and their Aza-analogues

A series of luotonin A homologues and their aza-analogues were prepared and evaluated their inhibitory activities on COX-1 and 2 as well as their selectivities on COX-2. The aza-analogue of dimethylene-bridged homologue of luotonin A,3,3’-dimethylene-2-(1’,8’-naphthyrid-2’-yl)-4(3H)-quinazolinone (2b), exhibited strongest inhibitory activity against COX-1 and COX-2 dependent phase of prostaglandin D2 generation in mouse bone marrow-derived mast cells in a concentration-dependent manner with an IC50 of 39.3 and 1.89μM, respectively. Selectivity of 2b on COX-2 over COX-1 was 21 which implied 2b can be a potential lead for the development of selective COX-2 inhibitor.