BROAD SPECTRUM BETA-LACTAMASE INHIBITORS

描述(改编自申请)：青霉素耐药细菌姿势 对人类福祉的严重威胁。这个项目将产生新的产品 旨在击败耐药微生物。最普遍的原因是 细菌耐药性涉及到用酶破坏抗生素 β-内酰胺酶。有超过255种已知的B-内酰胺酶，它们已经被 分成四个等级：A级到D级。历史上，A级是 临床上很重要。然而，C类介导性感染的发生率 在过去的十年里急剧增加。通常，这种抗药性感染可以 通过抗生素和B-内酰胺酶的联合应用而被击败 抑制剂。然而，目前商品化的β-内酰胺酶抑制剂是有效的 只能对抗A类酶。我们现在已经确定并申请了铅的专利 同时对A类和C类有效的化合物 β-内酰胺酶。这个项目将把这些线索发展成可行的商业 产品。与许多学术研究人员和 制药公司已经就位，允许访问代表 B-内酰胺酶以及这些抑制剂的微生物学评价。这个 目标是开发比商业产品更广泛的产品 抗生素/抑制剂组合。这将包括整体上更好的 针对临床重要疾病的亚类的活动或更好的活动 目前的商业产品没有针对的生物。 建议的商业应用： 这些抑制剂可以与商品化的β-内酰胺类抗生素联合使用，以扩大 抗生素的光谱。

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.