Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA.

Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA.
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DOI:
10.1016/j.bmcl.2008.09.041
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发表时间:
2008-10-15
影响因子:
2.7
通讯作者:
Gelb, Michael H.
Gelb, Michael H.
中科院分区:
医学4区
文献类型:
--
作者:
Oslund, Rob C.;Cermak, Nathan;Verlinde, Christophe L. M. J.;Gelb, Michael H.

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合成了YM-26734(一种已知的分泌型磷脂酶A2(sPLA 2)IIA组抑制剂)的简化类似物,发现其在低纳摩尔浓度下显示出强效抑制作用。类似物基于YM-26734的双十二烷酰基间苯三酚部分,其含有预测的活性位点钙结合基团。
Simplified analogs of YM-26734, a known inhibitor of secreted phospholipase A2 (sPLA2) group IIA were synthesized and found to display potent inhibition at low nanomolar concentrations. Analogs were based on the didodecanoylphloroglucinol portion of YM-26734 which contains the predicted active site calcium binding group.
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