单环β-内酰胺和铁载体模拟物的缀合物:专利评估(WO2023023393)。

IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Expert Opinion on Therapeutic Patents Pub Date : 2023-07-01 Epub Date: 2023-11-06 DOI:10.1080/13543776.2023.2262135
Alen Krajnc, Stanislav Gobec
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引用次数: 0

摘要

引言:β-内酰胺,包括单体酰胺,仍然是世界上最重要的一类抗生素。氨曲南是临床上唯一使用的单体菌,对许多革兰氏阴性菌具有显著的活性,但对一些最有问题的耐多药(MDR)病原体的活性有限,如耐多药铜绿假单胞菌和鲍曼不动杆菌共表达超广谱和金属β-内酰胺酶,它们可以通过水解灭活氨曲南。所涵盖的领域:声称结构新颖的铁载体偶联氨曲南衍生物对几种高度优先的病原体具有改进的抗菌性能。本发明报道了氨曲南的侧链延伸是可耐受的;氨基噻唑肟羧酸部分与铁载体模拟物的偶联显著提高了对几种有问题菌株的抗菌活性,包括具有碳青霉烯酶/头孢菌素酶活性的耐多药鲍曼分离株。专家意见:找到解决细菌对β-内酰胺类抗生素耐药性的新策略至关重要。考虑到β内酰胺是经过验证和安全的药物,这项研究可能会激发该领域在抗菌药物发现领域,特别是在铁载体模拟物方面发展新的想法。
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Conjugates of monocyclic β-lactams and siderophore mimetics: a patent evaluation (WO2023023393).

Introduction: β-Lactams, which include monobactams, remain the most important class of antibiotics worldwide. Aztreonam, the only monobactam in clinical use, has remarkable activity against many Gram-negative bacteria, but limited activity against some of the most problematic multidrug-resistant (MDR) pathogens, such as MDR Pseudomonas aeruginosa and Acinetobacter baumannii co-expressing extended-spectrum- and metallo-β-lactamases, which can inactivate aztreonam by hydrolysis.

Areas covered: Structurally novel siderophore-conjugated aztreonam derivatives with improved antibacterial properties against several high-priority pathogens are claimed. This invention reports that sidechain extension of aztreonam is tolerated; the coupling of its aminothiazoloxime carboxylic acid part with a siderophore mimetic significantly improved the antibacterial activity against several problematic strains, including MDR A. baumannii isolates with carbapenemase/cephalosporinase activity.

Expert opinion: Finding new strategies to tackle bacterial resistance to β-lactam antibiotics is critical. Considering that β lactams are validated and safe drugs, this research may stimulate the field to develop new ideas in the arena of antimicrobial drug discovery, particularly with respect to siderophore mimetics.

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来源期刊
CiteScore
12.10
自引率
1.50%
发文量
50
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.
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