A novel series of urea-based peptidomimetic calpain inhibitors.
A novel series of urea-based peptidomimetic calpain inhibitors.
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一系列新型的基于尿素的拟肽钙蛋白酶抑制剂。
DOI：
10.1016/j.bmcl.2005.12.068
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发表时间：
2006
期刊：
影响因子：
--
通讯作者：
Donkor,IsaacO
中科院分区：
文献类型：
--
作者：
Sanders,MLee;Donkor,IsaacO
合成了一系列P2位手性碳被氮取代的肽醛衍生物，作为μ-钙蛋白酶的脲基模拟肽抑制剂。这些化合物反映了肽醛钙蛋白酶抑制剂的一般SAR，但对μ-钙蛋白酶的选择性高于组织蛋白酶B。
A series of peptide aldehyde derivatives in which the P2chiral carbon has been replaced with nitrogen were synthesized as urea-based peptidomimetic inhibitors of μ-calpain. The compounds mirrored the general SAR of peptidyl aldehyde calpain inhibitors but displayed greater selectivity for μ-calpain over cathepsin B.