首页> 外文会议>the European Peptide Symposium >SYNTHESIS OF TRIFLUOROMETHYL KETONE-CONTAINING GLUTAMIC ACID AND GLUTAMINE PEPTIDES AS SEVERE ACUTE RESPIRATORY SYNDROME CORONAVIRUS 3CL PROTEASE INHIBITORS

【24h】

SYNTHESIS OF TRIFLUOROMETHYL KETONE-CONTAINING GLUTAMIC ACID AND GLUTAMINE PEPTIDES AS SEVERE ACUTE RESPIRATORY SYNDROME CORONAVIRUS 3CL PROTEASE INHIBITORS

机译：含三氟甲基酮谷氨酸和谷氨酰胺肽的合成重症急性呼吸综合征冠状病毒3CL蛋白酶抑制剂

获取原文

页面导航

摘要
著录项
相似文献
相关主题

摘要

Compounds containing a trifluoromethyl ketone moiety form an important group of biologically useful fluorinated molecules . A trifluoromethyl group that is a to the carbonyl functionality increases the electrophilicity of the carbonyl carbon, and therefore makes it prone to nucleophilic substitution by the cysteine residue which is present in the active site of cysteine proteases such as the severe acute respiratory syndrome coronavirus (SARS-CoV). This would lead to the formation of a tetrahedral adduct that is believed to mimic the intermediate formed during peptide-bond hydrolysis and suggests that compounds containing a trifluoromethyl ketone moiety may play an important role as SARS-CoV inhibitors . Based on these considerations, the synthesis of the peptides depicted in Scheme 1 (compounds 4 and 5) was embarked upon.

机译：含有三氟甲基酮部分的化合物形成了一组重要的生物学上有用的氟化分子。作为羰基官能团的三氟甲基增加了羰基碳的亲电性，因此使其易于通过半胱氨酸残基的亲核取代，其存在于半胱氨酸蛋白酶的活性位点，例如严重急性呼吸综合征冠状病毒（SARS -cov）。这将导致形成四面体加合物，据信模仿在肽 - 键水解过程中形成的中间体，并表明含有三氟甲基酮部分的化合物可以作为SARS-COV抑制剂发挥重要作用。基于这些考虑，开始了方案1中所示的肽（化合物4和5）的合成。

著录项

来源
《the European Peptide Symposium》|2007年||共2页
会议地点
作者
Magne O. Sydnes; Yoshio Hayashi; Vinay K. Sharma;
展开▼
作者单位

展开▼
会议组织
原文格式 PDF
正文语种
中图分类肽类;
关键词

相似文献

外文文献
中文文献
专利

1. Synthesis of glutamic acid and glutamine peptides possessing a trifluoromethyl ketone group as SARS-CoV 3CL protease inhibitors [J] . Sydnes MO, Hayashi Y, Sharma VK, Tetrahedron . 2006,第36期

机译：具有三氟甲基酮基的谷氨酸和谷氨酰胺肽的合成作为SARS-CoV 3CL蛋白酶抑制剂
2. Discovery, synthesis, and structure-based optimization of a series of N -(tert -Butyl)-2-(N -arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease [J] . Jacobs J., Grum-Tokars V., Zhou Y., Journal of Medicinal Chemistry . 2013,第2期

机译：发现，合成和基于结构的优化的一系列N-（叔丁基）-2-（N-芳酰胺基）-2-（吡啶-3-基）乙酰胺（ML188）作为有效的非共价小分子抑制剂严重急性呼吸综合征冠状病毒（SARS-CoV）3CL蛋白酶
3. Design and synthesis of cinanserin analogs as severe acute respiratory syndrome coronavirus 3CL protease inhibitors [J] . Yang QG, Chen LL, He XC, Chemical and Pharmaceutical Bulletin . 2008,第10期

机译：设计和合成cinanserin类似物作为严重急性呼吸综合征冠状病毒3CL蛋白酶抑制剂
4. SYNTHESIS OF TRIFLUOROMETHYL KETONE-CONTAINING GLUTAMIC ACID AND GLUTAMINE PEPTIDES AS SEVERE ACUTE RESPIRATORY SYNDROME CORONAVIRUS 3CL PROTEASE INHIBITORS [C] . Magne O. Sydnes, Yoshio Hayashi, Vinay K. Sharma the European Peptide Symposium . 2007

机译：含三氟甲基酮谷氨酸和谷氨酰胺肽的合成重症急性呼吸综合征冠状病毒3CL蛋白酶抑制剂
5. Design, synthesis and evaluation of severe acute respiratory syndrome coronavirus 3C-like protease inhibitors [D] . Zhang, Jianmin 2007

机译：严重急性呼吸综合征冠状病毒3C样蛋白酶抑制剂的设计，合成和评估
6. Synthesis of glutamic acid and glutamine peptides possessing a trifluoromethyl ketone group as SARS-CoV 3CL protease inhibitors [O] . Magne O. Sydnes, Yoshio Hayashi, Vinay K. Sharma, -1

机译：具有三氟甲基酮基的谷氨酸和谷氨酰胺肽的合成作为SARS-CoV 3CL蛋白酶抑制剂
7. Synthesis of glutamic acid and glutamine peptides possessing a trifluoromethyl ketone group as SARS-CoV 3CL protease inhibitors [O] . Magne O. Sydnes, Yoshio Hayashi, Vinay K. Sharma, 2006

机译：具有三氟甲基酮基的谷氨酸和谷氨酰胺肽作为SARS-COV 3CL蛋白酶抑制剂的合成

SYNTHESIS OF TRIFLUOROMETHYL KETONE-CONTAINING GLUTAMIC ACID AND GLUTAMINE PEPTIDES AS SEVERE ACUTE RESPIRATORY SYNDROME CORONAVIRUS 3CL PROTEASE INHIBITORS

摘要

著录项

相似文献

相关主题

期刊订阅