PEPTIDE SURROGATES IN RAPID SYNTHESIS OF HIV PROTEASE INHIBITORS

该子项目是利用 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。 考虑到生物分子中肽连接的普遍存在的性质，用生物分子中的电子等排体取代酰胺键是可行的。 潜在的候选药物一直是许多实验室的目标。成功的更换将提供更好的 稳定性、亲油性和吸收性。已经介绍了许多替代物，但其中许多替代物的合成 以组合的方式进行电子等排体是困难的并且需要几个步骤。因此，发现新的肽替代物， 更容易的合成是一项重要的成就，可以为研究含酰胺的 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.