PEPTIDE SURROGATES IN RAPID SYNTHESIS OF HIV PROTEASE INHIBITORS

这个子项目是许多研究子项目中的一个 由NIH/NCRR资助的中心赠款提供的资源。子项目和 研究者（PI）可能从另一个NIH来源获得主要资金， 因此可以在其他CRISP条目中表示。列出的机构是 中心，不一定是研究者的机构。 鉴于生物分子中普遍存在的肽键的性质，在潜在的候选药物中用电子等排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改善的稳定性、亲脂性和吸收。已经引入了许多替代物，但是以组合方式合成许多这些电子等排体是困难的，需要几个步骤。因此，发现新的肽替代物，更容易合成是一个重要的成就，可以打开新的机会，研究含酰胺的分子和开发具有新的物理化学性质的抑制剂。

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.