PEPTIDE SURROGATES IN RAPID SYNTHESIS OF HIV PROTEASE INHIBITORS

快速合成 HIV 蛋白酶抑制剂中的肽替代物

• 批准号: 7601717
• 负责人: CHI-HUEY WONG
• 金额: $ 0.76万
• 依托单位: UNIVERSITY OF CALIFORNIA, SAN DIEGO
• 依托单位国家: 美国
• 财政年份: 2007
• 资助国家: 美国
• 起止时间: 2007-05-01 至 2008-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7601717
• 关键词: Achievement; Amides; Biological; Computer Retrieval of Information on Scientific Projects Database; Development; Funding; Goals; Grant; Institution; Laboratories; Nature; Object Attachment; Peptides; Pharmaceutical Preparations; Property; Protease Inhibitor; Research; Research Personnel; Resources; Source; United States National Institutes of Health; absorption; combinatorial; improved; inhibitor/antagonist; lipophilicity; novel

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.

该子项目是利用该技术的众多研究子项目之一 资源由 NIH/NCRR 资助的中心拨款提供。子项目和 研究者 (PI) 可能已从 NIH 的另一个来源获得主要资金， 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。 鉴于生物分子中肽键的普遍存在，在潜在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更好的稳定性、亲脂性和吸收性。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物是困难的并且需要几个步骤。因此，发现更容易合成的新肽替代物是一项重要成就，可以为研究含酰胺分子和开发具有新颖理化性质的抑制剂开辟新的机会。