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약학회지 = Yakhak hoeji v.51 no.5, 2007년, pp.313 - 317  

새로운 계열의 선택적 COX-2 저해제: Luotonin A 동족체 및 그 질소 유도체
A New Class of Selective COX-2 Inhibitor: Luotonin A Homologues and their Aza-analogues

김동현   (영남대학교 약학대학UU0000951  ); 량경록   (영남대학교 약학대학UU0000951  ); 오준석   (영남대학교 약학대학UU0000951  ); 장영동   (영남대학교 약학대학UU0000951  ); 김진철   (영남대학교 약학대학UU0000951  ); 홍태균   (영남대학교 약학대학UU0000951  ); 황남경   (영남대학교 약학대학UU0000951  ); 정환기   (영남대학교 약학대학UU0000951  ); 김윤경   (영남대학교 약학대학UU0000951  ); 장현욱   (영남대학교 약학대학UU0000951  );
  • 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 $D_2$ 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.


  • 주제어

    luotonin A .   COX-2 inhibitor .   bone marrow-derived mast cell .   prostagladin $D_2$ .   3,3'-dimethylene-2-(quinolin-2'-yl)-4(3H)-quinazolinone .   3,3'-dimethylene-2-(1',8'-naphthyrid-2'-yl)-4(3H)-quinazolinone.  

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