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primary topic: Disarming superbugs: New frontiers in inhibiting NDM-1 and other clinically relevant metallo-β-lactamases

Disarming superbugs: New frontiers in inhibiting NDM-1 and other clinically relevant metallo-β-lactamases
type: AcademicArticle
type: Article
abstract: The emergence and global spread of Metallo-β-lactamases (MBLs), particularly New Delhi Metallo-β-lactamase (NDM), Verona Integron-encoded Metallo-β-lactamase (VIM), and Imipenemase (IMP), pose a significant threat to the efficacy of β-lactam antibiotics, including carbapenems, often regarded as the last line of defence against multidrug-resistant bacterial infections. This review comprehensively analyzes recent advances in the development of MBL inhibitors (MBLIs), targeting NDM, VIM, and IMP enzymes with a special focus on NDM-1. The inhibitors are categorized based on key functional groups responsible for their activity, offering insight into the structure activity relationships (SAR) that govern their potency and selectivity. We highlight representative compounds with potent inhibition data (IC50/Ki values), supported by molecular docking studies and where available co-crystal structures with target MBLs to elucidate their binding interactions. Synthetic approaches for these inhibitors are also discussed. This review aims to provide a detailed, functionally organized framework for ongoing efforts in designing potent, broad-spectrum MBL inhibitors capable of restoring the utility of β-lactam antibiotics.
date: 2025
volume: 301
issue: 118220
status: peerReviewed
status: published
author list: authors
type: EPrint
type: ArticleEPrint
is part of: repository
subject: QR Microbiology

Elsevier BV
type: Organization

Eur. J. Med. Chem.
type: Collection

Aayushi Saini
type: Person
given name: Aayushi
family name: Saini

Ankita Pundir
type: Person
given name: Ankita
family name: Pundir

Vinod D Chaudhari
type: Person
given name: Vinod D
family name: Chaudhari

Amit Patwa
type: Person
given name: Amit
family name: Patwa

Pulkit Dhiman
type: Person
given name: Pulkit
family name: Dhiman

Manoj D Dhole
type: Person
given name: Manoj D
family name: Dhole

Arya B Narayanan
type: Person
given name: Arya B
family name: Narayanan

HTML Summary of #3219 Disarming superbugs: New frontiers in inhibiting NDM-1 and other clinically relevant metallo-β-lactamases
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primary topic: Disarming superbugs: New frontiers in inhibiting NDM-1 and other clinically relevant metallo-β-lactamases

QR Microbiology
type: Concept