首页 | 本学科首页   官方微博 | 高级检索  
   检索      


New methods for solid phase peptide synthesis of transitionstate analog inhibitors of HIV-1 protease and DPP-IV
Authors:Jan Piron and Dirk Tourwé
Institution:(1) Organic Chemistry, Free University of Brussels, Pleinlaan 2, B-1050 Brussels, Belgium
Abstract:Summary A new and stereoselective method to synthesize hydroxyethylamine and hydroxymethylamide peptide bond isosteres is developed. The key step is the addition of 2-trimethylsilylthiazole to agr-aminoaldehydes, followed by transformation to agr-hydroxy-beta-aminoaldehydes. The stereochemistry of the addition can be manipulated by the choice of the nitrogen substitution. The isosteres are easily synthesized via Solid Phase Peptide Synthesis, which rapidly gives the desired pseudopeptides.
Keywords:Hydroxyethylamine isostere  Hydroxymethylamide isostere  2-Substituted thiazoles
本文献已被 SpringerLink 等数据库收录!
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号