Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors
Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors
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DOI：
10.1016/s0960-894x(99)00587-9
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发表时间：
2000-01-03
影响因子：
2.7
通讯作者：
Worland, ST
中科院分区：
文献类型：
--
作者：
Dragovich, PS;Zhou, R;Worland, ST
三肽衍生的分子纳入C-末端酮亲电体进行了评价，作为可逆的抑制剂的含半胱氨酸的人鼻病毒3C蛋白酶（3CP）。当针对HRV血清型-14测试时，这种化合物的优化实例显示出有效的3CP抑制活性（Ki = 0.0045 μ M）和体外抗病毒性质（EC 50 = 0.34 μ M）。(C)1999 Elsevier Science Ltd.保留所有权利。
Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). An optimized example of such compounds displayed potent 3CP inhibition activity (K-i = 0.0045 mu M) and in vitro antiviral properties (EC50 = 0.34 mu M) when tested against HRV serotype-14. (C) 1999 Elsevier Science Ltd. All rights reserved.