New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CLpro inhibitors

New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CLpro inhibitors
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DOI:
10.1016/j.bmcl.2009.03.118
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发表时间:
2009-05-15
影响因子:
2.7
通讯作者:
Kiso, Yoshiaki
Kiso, Yoshiaki
中科院分区:
医学4区
文献类型:
--
作者:
Regnier, Thomas;Sarma, Diganta;Kiso, Yoshiaki

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合成了一系列含三氟甲基、苯并噻唑基或噻唑基酮的多肽类化合物作为SARS CoV 3CL蛋白酶抑制剂,并通过体外蛋白酶抑制试验评价了它们的活性。三个候选化合物在开发新的抗SARS化合物方面取得了令人鼓舞的结果。(C)2009爱思唯尔有限公司保留所有权利。
A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds. (C) 2009 Elsevier Ltd. All rights reserved.