BROAD SPECTRUM BETA-LACTAMASE INHIBITORS

广谱 β-内酰胺酶抑制剂

• 批准号: 6294170
• 负责人: JOHN D BUYNAK
• 金额: $ 16.02万
• 依托单位: ALAMX, LLC
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-06-01 至 2003-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6294170
• 关键词: antibiotics; bacterial disease; beta lactamase; chemical registry /resource; drug design /synthesis /production; drug interactions; drug resistance; enzyme inhibitors

DESCRIPTION (Adapted from the application): Penicillin-resistant bacteria pose a serious threat to human welfare. This project will generate new products designed to defeat resistant microorganisms. The most prevalent cause of bacterial resistance involves the destruction of the antibiotic with the enzyme B-lactamase. There are more than 255 known B-lactamases, which have been grouped into four classes: A through D. Historically, class A has been the most clinically important. However, the incidence of class C-mediated infections has increased dramatically in the past decade. Often such resistant infections can be defeated through the co-administration of an antibiotic and a B-lactamase inhibitor. However, current commercial B-lactamase inhibitors are effective only against class A enzymes. We have now identified and patented lead compounds which are simultaneously effective against both class A and class C B-lactamases. This project will develop those leads into viable commercial products. Collaborations with a number of academic researchers and pharmaceutical companies are in place, allowing access to representative B-lactamases as well as microbiological evaluations of these inhibitors. The objective is to develop products which have a broader spectrum than commercial antibiotic/inhibitor combinations. This will include either better overall activity or better activity against a subclass of clinically important organisms not targeted by current commercial products. PROPOSED COMMERCIAL APPLICATION: These inhibitors can be combined with the commercial beta-lactam antibiotic to broaden the spectrum of the antibiotic.

描述（改编自应用程序）：青霉素耐药菌构成 严重威胁人类福祉。该项目将产生新产品 旨在击败耐药微生物。的最普遍原因 细菌的耐药性包括酶对抗生素的破坏 β-内酰胺酶已知有超过255种β-内酰胺酶， 分为四类：A到D。从历史上看，A类是最多的 临床上很重要。然而，C类介导的感染的发生率 在过去的十年里急剧增加。通常这种耐药感染可以 通过抗生素和β-内酰胺酶的联合给药被击败 抑制剂.然而，目前商业化的β-内酰胺酶抑制剂是有效的， 只能对抗A类酶我们已经鉴定出铅并申请了专利 同时有效对抗A类和C类的化合物 β-内酰胺酶该项目将把这些线索发展成可行的商业 产品.与一些学术研究人员合作， 制药公司已经到位，允许进入代表 β-内酰胺酶以及这些抑制剂的微生物学评价。的 我们的目标是开发具有比商业更广泛的频谱的产品。 抗生素/抑制剂组合。这将包括更好的整体 活性或更好的活性，针对临床重要的亚类 目前商业产品不针对的微生物。 拟定商业应用： 这些抑制剂可以与商业β-内酰胺抗生素组合，以拓宽 抗生素的光谱。