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새로운 계열의 선택적 COX-2 저해제: Luotonin A 동족체 및 그 질소 유도체
김동현,량경록,오준석,장영동,김진철,홍태균,황남경,정환기,김윤경,장현욱,Kim, Dong-Hyeon,Liang, Jing-Liu,Oh, Joon-Seok,Jahng, Yurng-Dong,Kim, Jin-Cheul,Hong, Tae-Gyun,Hwang, Nam-Kyung,Chung, Hwan-Ki,Kim, Yun-Kyung,Chang, Hyeun-Wook 대한약학회 2007 약학회지 Vol.51 No.5
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 $D_2$ generation in mouse bone marrow-derived mast cells in a concentration-dependent manner with an $IC_{50}$ of 39.3 and $1.89{\mu}M$, 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.