锥虫半胱氨酸蛋白酶克氏锥虫蛋白酶的强效第二代乙烯基磺酰胺抑制剂。
Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain.
作者信息
Roush W R, Cheng J, Knapp-Reed B, Alvarez-Hernandez A, McKerrow J H, Hansell E, Engel J C
机构信息
Department of Chemistry, University of Michigan, Ann Arbor, 48109, USA.
出版信息
Bioorg Med Chem Lett. 2001 Oct 22;11(20):2759-62. doi: 10.1016/s0960-894x(01)00566-2.
Abstract
A new family of potent N-alkoxyvinylsulfonamide inhibitors of cruzain have been developed. Inhibitor 13 has a second order inactivation rate constant of 6,480,000s(-1)M(-1) versus cruzain, and is also highly effective against Trypanosoma cruzi trypomastigotes in a tissue culture assay.
摘要
已开发出一类新型的强效克鲁兹蛋白酶N-烷氧基乙烯基磺酰胺抑制剂。抑制剂13与克鲁兹蛋白酶的二级失活速率常数为6480000s⁻¹M⁻¹，并且在组织培养试验中对克氏锥虫锥鞭毛体也具有高效性。
Zotero 插件