Lead optimization of new antibacterials/antimalarials that target ACP synthase

针对 ACP 合酶的新型抗菌/抗疟药的先导优化

• 批准号: 398103-2011
• 负责人: Byers, David
• 金额: $ 5.59万
• 依托单位: Dalhousie University
• 依托单位国家: 加拿大
• 项目类别: Collaborative Health Research Projects
• 财政年份: 2011
• 资助国家: 加拿大
• 起止时间: 2011-01-01 至 2012-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=487682
• 关键词: Lead; optimization; new; antibacterials; antimalarials

This project focuses on producing new antibiotic drugs that are "broad-spectrum" to treat all types of drug-resistant bacterial infections as well as, potentially, tuberculosis and malaria. Drug resistance is a growing problem that has made current antibiotics much less effective than before. This is of special concern in resistant strains of Staph. aureus (the "superbug" MRSA); Gram-negative infections caused by E. coli; so-called "XDR" tuberculosis caused by strains of Mycobacterium tuberculosis; and malaria, the causative agent of which is Pl. falciparum. All of these diverse diseases can be targeted by the same drug, provided the mechanism of action is present in all of them. This proposal uses novel compounds that kill MRSA, developed in previous work, as a starting point for making such broad-spectrum antibiotics. Our compounds target ACP

该项目的重点是生产新的抗生素药物，这些药物是“广谱”的，可以治疗所有类型的耐药细菌感染，以及潜在的结核病和疟疾。耐药性是一个日益严重的问题，使目前的抗生素比以前有效得多。这在葡萄球菌的耐药菌株中特别令人关注。金黄色葡萄球菌（“超级细菌”MRSA）;大肠杆菌;由结核分枝杆菌菌株引起的所谓的“XDR”结核;以及疟疾，其病原体是Pl.恶性疟原虫。所有这些不同的疾病都可以被同一种药物靶向，只要它们的作用机制都存在。这项提案使用了在以前的工作中开发的杀死MRSA的新化合物，作为制造这种广谱抗生素的起点。我们的化合物靶向ACP