In 2012,Li, Xianfeng; Liu, Yang; Zhang, Yong-Kang; Plattner, Jacob J.; Baker, Stephen J.; Bu, Wei; Liu, Liang; Zhou, Yasheen; Ding, Charles Z.; Zhang, Suoming; Kazmierski, Wieslaw M.; Hamatake, Robert; Duan, Maosheng; Wright, Lois L.; Smith, Gary K.; Jarvest, Richard L.; Ji, Jing-Jing; Cooper, Joel P.; Tallant, Matthew D.; Crosby, Renae M.; Creech, Katrina; Wang, Amy published 《Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups》.Bioorganic & Medicinal Chemistry Letters published the findings.Product Details of 16982-21-1 The information in the text is summarized as follows:
We have synthesized and evaluated a series of novel HCV NS3 protease inhibitors with various P4 capping groups, which include urea, carbamate, methoxy-carboxamide, cyclic carbamate and amide, pyruvic amide, oxamate, oxalamide and cyanoguanidine. Most of these compounds are remarkably potent, exhibiting single-digit to sub-nanomolar activity in the enzyme assay and cell-based replicon assay. Selected compounds were also evaluated in the protease-inhibitor-resistant mutant transient replicon assay, and they were found to show quite different potency profiles against a panel of HCV protease-inhibitor-resistant mutants. The results came from multiple reactions, including the reaction of Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Product Details of 16982-21-1)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Product Details of 16982-21-1
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics