title: Disarming superbugs: New frontiers in inhibiting NDM-1 and other clinically relevant metallo-β-lactamases
creator: Dhiman, Pulkit
creator: Patwa, Amit
creator: Narayanan, Arya B
creator: Saini, Aayushi
creator: Pundir, Ankita
creator: Dhole, Manoj D
creator: Chaudhari, Vinod D
subject: QR Microbiology
description: 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.
publisher: Elsevier BV
date: 2025
type: Article
type: PeerReviewed
identifier:   Dhiman, Pulkit and Patwa, Amit and Narayanan, Arya B and Saini, Aayushi and Pundir, Ankita and Dhole, Manoj D and Chaudhari, Vinod D  (2025) Disarming superbugs: New frontiers in inhibiting NDM-1 and other clinically relevant metallo-β-lactamases.  Eur. J. Med. Chem., 301 (118220).  p. 118220.      
relation: http://crdd.osdd.net/open/3219/