PENICILLIN-DERIVED INHIBITORS

青霉素衍生抑制剂

• 批准号: 7355222
• 负责人: JOHN D BUYNAK
• 金额: $ 0.04万
• 依托单位: WASHINGTON UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2006
• 资助国家: 美国
• 起止时间: 2006-02-01 至 2007-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7355222
• 关键词: PENICILLIN; DERIVED; INHIBITORS

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. The synthesis and b-lactamase inhibitory activity of four 6-(mercaptomethyl)penicillinates and the four corresponding 6-(hydroxymethyl)penicillinates are described. These penicillins include both C6 stereoisomers as well as the sulfide and sulfone oxidn. states of the penam thiazolidine sulfur. All compounds were evaluated as inhibitors of representative metallo- and serine-b-lactamases enzymes. Selected (mercaptomethyl)penicillinates are shown to inactivate both metallo- and serine-b-lactamases and to display synergism with piperacillin against b-lactamase producing strains.

这个子项目是利用由NIH/NCRR资助的中心拨款提供的资源的许多研究子项目之一。子项目和调查员(PI)可能从另一个NIH来源获得了主要资金，因此可能会出现在其他CRISE条目中。列出的机构是针对中心的，而不一定是针对调查员的机构。报道了4种6-(巯甲基)青霉酸酯及其对应的4种6-羟甲基青霉酸酯的合成及其对β-内酰胺酶的抑制活性。这些青霉素既包括C6立体异构体，也包括硫化物和砜氧化物。四氢呋喃硫磺的状态。所有化合物都被评估为具有代表性的金属和丝氨酸-b-内酰胺酶的抑制剂。经筛选的(硫代甲基)青霉酸酯对金属和丝氨酸-b-内酰胺酶均有灭活作用，并与哌拉西林对产酶菌株有协同作用。