PEPTIDE SURROGATES IN RAPID SYNTHESIS OF HIV PROTEASE INHIBITORS

本子项目是利用由NIH/NCRR资助的中心赠款提供的资源的众多研究子项目之一。子项目和研究者（PI）可能已经从另一个NIH来源获得了主要资金，因此可以在其他CRISP条目中表示。列出的机构是中心的，不一定是研究者的机构。鉴于肽链在生物分子中无处不在的性质，在潜在的候选药物中用同位体取代酰胺键一直是许多实验室的持续目标。成功的替代品将提供更好的稳定性、亲脂性和吸收率。许多替代物已经被引入，但是以组合的方式合成这些同分异构体是困难的，需要几个步骤。因此，发现新的更容易合成的肽替代物是一项重要的成就，它可以为研究含酰胺分子和开发具有新型物理化学性质的抑制剂开辟新的机会。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Given the ubiquitous nature of the peptide linkage in biological molecules, replacement of the amide bond with isosteres in potential drug candidates has been a continual goal of many laboratories. Successful replacements will provide improved stability, lipophilicity, and absorption. Many surrogates have been introduced already, yet the synthesis of many of these isosteres in a combinatorial way is difficult and requires several steps. Thus, the discovery of new peptide surrogates with easier syntheses is an important achievement that could open new opportunities for the study of amide-containing molecules and the development of inhibitors with novel physicochemical properties.