Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain

Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain
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DOI:
10.1016/s0960-894x(01)00566-2
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发表时间:
2001-10-22
影响因子:
2.7
通讯作者:
Engel, JC
Engel, JC
中科院分区:
医学4区
文献类型:
--
作者:
Roush, WR;Cheng, JM;Engel, JC

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新发现了一类有效的N-alkoxyvinylsulfonamide cruzain抑制剂,抑制剂13对cruzain具有6,480,000 s(-1) M-1的二级失活速率常数,并且在组织培养实验中对克氏锥虫(Trypanosoma cruzi)也非常有效。2001爱思唯尔科学有限公司版权所有。
A new family of potent N-alkoxyvinylsulfonamide inhibitors of cruzain have been developed, Inhibitor 13 has a second order inactivation rate constant of 6,480,000 s(-1) M-1 versus cruzain, and is also highly effective against Trypanosoma cruzi trypomastigotes in a tissue culture assay. (C) 2001 Elsevier Science Ltd. All rights reserved.