Structural variations in keto-glutamines for improved inhibition against hepatitis A virus 3C proteinase
Structural variations in keto-glutamines for improved inhibition against hepatitis A virus 3C proteinase
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DOI：
10.1016/j.bmcl.2004.05.021
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发表时间：
2004-07-16
影响因子：
2.7
通讯作者：
Vederas, JC
中科院分区：
文献类型：
--
作者：
Jain, RP;Vederas, JC
合成了一系列在β-碳上具有R和S构型的酮基-谷氨酰胺四肽类似物，其含有2-氧代-吡咯烷环作为谷氨酰胺侧链模拟物。带有邻苯二甲酰肼部分的化合物在低微摩尔范围内显示出改善的HAV 3C蛋白酶的可逆抑制。(C)2004爱思唯尔有限公司保留所有权利。
A series of keto-glutamine tetrapeptide analogs containing a 2-oxo-pyrrolidine ring as a glutamine side chain mimic were synthesized with both R and S configuration at the beta-carbon. Compounds bearing a phthalhydrazide moiety show improved reversible inhibition of HAV 3C proteinase in the low micromolar range. (C) 2004 Elsevier Ltd. All rights reserved.