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

• 영문명: A New Class of S elective COX-2 Inhibitor: Luotonin A Homoligues and their Aza-analogues
• 발행기관: 대한약학회
• 저자명: 김동현(Dong Hyeon Kim) 량경록(Jing Liu Liang) 오준석(Joon Seok Oh) 장영동(Yurng Dong Jahng) 김진철(Jin Cheul Kim) 홍태균(Tae Gyun Hong) 황남경(Nam Kyung Hwang) 정환기(Hwan Ki Chung) 김윤경(Yun Kyung Kim) 장현욱(Hyeun Wook Chang)
• 간행물 정보: 『약학회지』제51권 제5호 (2007년), 313~317쪽, 전체 5쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2007.10.31

영문 초록

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.

키워드

luotonin A COX-2 inhibitor bone marrow-derived mast cell prostagladin D2 3,3'-dimethylene-2-(quinolin-2'-yl)-4(3H)-quinazolinone 3,3'-dimethylene-2-(1',8'-naphthyrid-2'-yl)-4(3H)-quinazolinone