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新型阿格拉丁A类似物的合成,这些类似物显示出比天然产物更强的基质金属蛋白酶(MMP)-12抑制活性。

Synthesis of novel ageladine A analogs showing more potent matrix metalloproteinase (MMP)-12 inhibitory activity than the natural product.

作者信息

Ando Naoki, Terashima Shiro

机构信息

Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd, 2399-1, Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan.

出版信息

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5461-3. doi: 10.1016/j.bmcl.2009.07.099. Epub 2009 Jul 23.

Abstract

By employing a previously established synthetic scheme, the synthesis described in the title was carried out in order to explore the substituent effects in the pyrrole ring of ageladine A on MMP-12 inhibitory activity. It became evident that a halogen atom (Br or Cl) at the 2-position and an additional bromine atom at the 4-position are highly effective for improving the inhibitory activity. These studies led us to discover three novel ageladine A analogs (4a, c, o) showing more potent MMP-12 inhibitory activity than the natural product.

摘要

通过采用先前建立的合成方案,进行了标题中所述的合成,以探究阿格拉定A吡咯环上的取代基对基质金属蛋白酶-12(MMP-12)抑制活性的影响。结果表明,2-位的卤原子(Br或Cl)和4-位的额外溴原子对提高抑制活性非常有效。这些研究使我们发现了三种新型阿格拉定A类似物(4a、c、o),它们对MMP-12的抑制活性比天然产物更强。

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