Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain
Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain
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DOI：
10.1016/s0960-894x(03)00756-x
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发表时间：
2003-10-20
影响因子：
2.7
通讯作者：
Chibale, K
中科院分区：
文献类型：
--
作者：
Chiyanzu, I;Hansell, E;Chibale, K
虽然商业靛红对靶蛋白酶几乎没有活性，但发现缩氨基硫脲衍生物具有活性。该系列中活性最强的化合物显示出对罗地蛋白酶的抑制IC 50值为1 μ M。发现一种缩氨基硫脲对所有三种蛋白酶都有活性，其抑制IC 50值为10 μ M或更低。通常发现，在靛红支架的芳香部分上N-苄基化和适当取代的组合对于酮抑制剂特别是对抗cruzain是有益的。(C)2003 Elsevier Ltd.保留所有权利。
While commercial isatins were practically inactive against the target proteases, thiosemicarbazone derivatives were found to be active. The most active compound from the series displayed an inhibitory IC50 value of 1 muM against rhodesain. One thiosemicarbazone was found to be active against all three proteases with inhibitory IC50 values of 10 muM or less. A combination of N-benzylation and appropriate substitution on the aromatic portion of the isatin scaffold was generally found to be beneficial especially against cruzain for ketone inhibitors. (C) 2003 Elsevier Ltd. All rights reserved.