Novel type of plasmin inhibitors: Providing insight into P4 moiety and alternative scaffold to pyrrolopyrimidine.
Novel type of plasmin inhibitors: Providing insight into P4 moiety and alternative scaffold to pyrrolopyrimidine.
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新型纤溶酶抑制剂：深入了解 P4 部分和吡咯并嘧啶的替代支架。
DOI：
10.1016/j.bmc.2015.04.013
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发表时间：
2015
期刊：
影响因子：
--
通讯作者：
Y. Yamashita.
中科院分区：
文献类型：
--
作者：
N. Teno;K;Gohda;K. Wanaka;Y. Tsuda;M. Akagawa;E. Akiduki;M. Araki;Masuda A. Masuda;T. Otsubo;Y. Yamashita.
在这里，我们报告了一系列的纤溶酶抑制剂，最初是从母体结构的1和2。我们的工作集中在2的P4部分的优化和在母体化合物中寻找吡咯并嘧啶的替代支架上。前者的结果为进一步优化纤溶酶抑制剂中的P4部分提供了关键信息，后者的结果显示，从苯并咪唑支架延伸的适当部分与纤溶酶活性位点中的S4口袋接合。
Here we report a series of plasmin inhibitors which were originally derived from the parent structure of1and2. Our efforts focused on the optimization of the P4 moiety of2and on the quest of alternative scaffold to pyrrolopyrimidine in the parent compounds. The results of the former gave us pivotal information on the further optimization of the P4 moiety in plasmin inhibitors and those of the latter revealed that appropriate moieties extending from the benzimidazole scaffold engaged with S4 pocket in the active site of plasmin.