YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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A New Class of Selective COX-2 Inhibitor: Luotonin A Homologues and their Aza-analogues

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

  • Published : 2007.10.31
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Abstract

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.

Keywords

References

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