PEPTIDE SURROGATES IN RAPID SYNTHESIS OF HIV PROTEASE INHIBITORS

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 鉴于生物分子中多肽连接的无处不在的性质，在潜在的候选药物中用异构体取代酰胺键一直是许多实验室的持续目标。成功的替代将提供更好的稳定性、亲脂性和吸收能力。已经引入了许多替代物，但以组合方式合成许多这些异构体是困难的，并且需要几个步骤。因此，发现更容易合成的新的多肽替代品是一项重要的成就，可能为含酰胺分子的研究和具有新的物理化学性质的抑制剂的开发打开新的机会。

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.