Explanipedia

Furocoumarin Analogs from Radix Angelica Dahurica Confer Inhibitory Efficacy Against New Delhi Metallo-Β-Lactamase-1 Open

Le Zhai, Yiqiang Wu, Yi-Xue Wang, Yao Zhao, Huaping Xie , et al. · 2025

Discovery of hydroxamate as a promising scaffold dually inhibiting metallo- and serine-β-lactamases Open

Xiaorong Wu, Weiya Chen, Lu Liu, Ke‐Wu Yang · 2023

CCDC 2216318: Experimental Crystal Structure Determination Open

T. Cheng, Jing Ji, C. -Y. Yang, Dan Nie, Ke‐Wu Yang , et al. · 2023

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …

A Modified Vancomycin Molecule Confers Potent Inhibitory Efficacy against Resistant Bacteria Mediated by Metallo-β-Lactamases Open

Le Zhai, Ya Liu, Yue Jiang, Ling-Yan Kong, Jian Xiao , et al. · 2022

Multidrug-resistant bacterial infections mediated by metallo-β-lactamases (MβLs) have grown into an emergent health threat, and development of novel antimicrobials is an ideal strategy to combat the infections. Herein, a novel vancomycin d…

Self-Assembled Cationic Nanoparticles Combined with Curcumin against Multidrug-Resistant Bacteria Open

Jian-Bin Zhen, Jiajia Yi, Huan Ding, Ke‐Wu Yang · 2022

The overuse of antibiotics exacerbates the development of antibiotic-resistant bacteria, threatening global public health, while most traditional antibiotics act on specific targets and sterilize through chemical modes. Therefore, it is a …

Hydroxamate and thiosemicarbazone: Two highly promising scaffolds for the development of SARS-CoV-2 antivirals Open

Yin‐Sui Xu, Jia‐Zhu Chigan, Jiaqi Li, Huanhuan Ding, Le-Yun Sun , et al. · 2022

Discovery of Environment-Sensitive Fluorescent Probes for Detecting and Inhibiting Metallo-Β-Lactamase Open

Cheng Chen, Cheng Chen, Yang K. Xiang, May D. Wang, Nana Wang , et al. · 2022

CCDC 2051560: Experimental Crystal Structure Determination Open

Jia‐Zhu Chigan, Jiaqi Li, Huanhuan Ding, Yin‐Sui Xu, Lu Liu , et al. · 2021

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …

Ebsulfur and Ebselen as highly potent scaffolds for the development of potential SARS-CoV-2 antivirals Open

Le-Yun Sun, Cheng Chen, Jian-Peng Su, Jiaqi Li, Zhihui Jiang , et al. · 2021

Dipyridyl-substituted thiosemicarbazone as a potent broad-spectrum inhibitor of metallo-β-lactamases Open

Jiaqi Li, Han Gao, Le Zhai, Le-Yun Sun, Cheng Chen , et al. · 2021

A Degradation Product from Hydrolysate of Imipenem with Imis Broad-Spectrum Inhibits Metallo-β-Lactamases Open

Ying Ge, Li-Wei Xu, Jian-Bin Zhen, Cheng Chen, Miao Lv , et al. · 2020

Background: Infections caused by metallo-β-lactamases (MβLs)-producing antibiotic-resistant bacteria pose a severe threat to public health. The synergistic use of current antibiotics in combination with MβL inhibitors is a promising therap…

Binding of 2-(Triazolylthio)acetamides to Metallo-β-lactamase CcrA Determined with NMR Open

Hanna Andersson, Patrik Jarvoll, Shao-Kang Yang, Ke‐Wu Yang, Máté Erdélyi · 2020

Metallo-β-lactamase (MBL)-producing bacteria resistant to β-lactam antibiotics are a serious threat to human health. Despite great efforts and important progress in the discovery of MBL inhibitors (MBLIs), there is none in clinical use. He…

Synthesis and Bioactivity of Thiazolethioacetamides as Potential Metallo-β-Lactamase Inhibitors Open

Yilin Zhang, Yong Yan, Xuejun Wang, Ke‐Wu Yang · 2020

Metallo-β-lactamase (MβLs) mediated antibiotic resistance seriously threatens the treatment of bacterial diseases. Recently, we found that thioacetamides can be a potential MβL inhibitor skeleton. In order to improve the information of the…

Kinetic, Thermodynamic, and Crystallographic Studies of 2-Triazolylthioacetamides as Verona Integron-Encoded Metallo-β-Lactamase 2 (VIM-2) Inhibitor Open

Xiang Yang, Yuejuan Zhang, Ying Ge, Yajun Zhou, Cheng Chen , et al. · 2020

Inhibition of β-lactamases presents a promising strategy to restore the β-lactams antibacterial activity to resistant bacteria. In this work, we found that aromatic carboxyl substituted 2-triazolylthioacetamides 1a–j inhibited VIM-2, exhib…

<i>meta</i>-Substituted benzenesulfonamide: a potent scaffold for the development of metallo-β-lactamase ImiS inhibitors Open

Ya Liu, Cheng Chen, Le-Yun Sun, Han Gao, Jian-Bin Zhen , et al. · 2020

Meta-substituted benzenesulfonamides specifically inhibit metallo-β-lactamase ImiS with an IC₅₀ value ranging from 0.11 to 0.86 μM.

Dithiocarbamate as a Valuable Scaffold for the Inhibition of Metallo-β-Lactmases Open

Ying Ge, Li-Wei Xu, Ya Liu, Le-Yun Sun, Han Gao , et al. · 2019

The ‘superbug’ infection caused by metallo-β-lactamases (MβLs) has grown into an emergent health threat. Given the clinical importance of MβLs, a novel scaffold, dithiocarbamate, was constructed. The obtained molecules, DC1, DC8 and DC10, …

Halogen-Substituted Triazolethioacetamides as a Potent Skeleton for the Development of Metallo-β-Lactamase Inhibitors Open

Yilin Zhang, Yong Yan, Lufan Liang, Jie Feng, Xuejun Wang , et al. · 2019

Metallo-β-lactamases (MβLs) are the target enzymes of β-lactam antibiotic resistance, and there are no effective inhibitors against MβLs available for clinic so far. In this study, thirteen halogen-substituted triazolethioacetamides were d…

Amino Acid Thioesters Exhibit Inhibitory Activity against B1–B3 Subclasses of Metallo-β-lactamases Open

Yuejuan Zhang, Xiaolong Liu, Wenming Wang, Cheng Chen, Mu-Han Zhao , et al. · 2019

Superbug infection caused by metallo-β-lactamases (MβLs) is a global public health threat. Previous studies reported that the thioesters specifically inhibited the B3 subclass MβL L1. In this work, nine amino acid thioesters 1-9 were synth…

Thermokinetic profile of NDM-1 and its inhibition by small carboxylic acids Open

Qian Wang, Yuan He, Rui Lu, Wenming Wang, Ke‐Wu Yang , et al. · 2018

The New Delhi metallo-β-lactamase (NDM-1) is an important clinical target for antimicrobial research, but there are insufficient clinically useful inhibitors and the details of NDM-1 enzyme catalysis remain unclear. The aim of this work is…

Carbamylmethyl Mercaptoacetate Thioether: A Novel Scaffold for the Development of L1 Metallo-β-lactamase Inhibitors Open

Yanan Chang, Xiang Yang, Yuejuan Zhang, Wenming Wang, Cheng Chen , et al. · 2017

Given the clinical importance of metallo-β-lactamases (MβLs), a new scaffold, N-substituted carbamylmethyl mercaptoacetate thioether, was constructed. The obtained molecules 1-16 inhibited MβLs from all three subclasses, but …

Triazolylthioacetamide: A Valid Scaffold for the Development of New Delhi Metallo-β-Lactmase-1 (NDM-1) Inhibitors Open

Le Zhai, Yilin Zhang, Joon S. Kang, Peter Oelschlaeger, Lin Xiao , et al. · 2016

The metallo-β-lactamases (MβLs) cleave the β-lactam ring of β-lactam antibiotics, conferring resistance against these drugs to bacteria. Twenty-four triazolylthioacetamides were prepared and evaluated as inhibitors of representatives of th…

Antibacterial Fischer Carbenoid CO-Releasing Molecules Open

Ling-Ling Zhou, Yaqing Zhou, Yanli Tang, Ke‐Wu Yang, Lei Zhang , et al. · 2016

水溶性差的关键问题, 发展了一类离子型 Fischer 卡宾类 CORM 先导结构

Amino Acid Thioester Derivatives: A Highly Promising Scaffold for the Development of Metallo-β-lactamase L1 Inhibitors Open

Xiaolong Liu, Ying Shi, Joon S. Kang, Peter Oelschlaeger, Ke‐Wu Yang · 2015

In light of the biomedical significance of metallo-β-lactamases (MβLs), ten new mercaptoacetic acid thioester amino acid derivatives were synthesized and characterized. Biological activity assays indicated that all these synthesized compou…

Azolylthioacetamide: A Highly Promising Scaffold for the Development of Metallo-β-lactamase Inhibitors Open

Shao-Kang Yang, Joon S. Kang, Peter Oelschlaeger, Ke‐Wu Yang · 2015

A new scaffold, azolylthioacetamide, was constructed and assayed against metallo-β-lactamases (MβLs). The obtained molecules specifically inhibited MβL ImiS, and 1c was found to be the most potent inhibitor, with a K i = 1.2 μM using imipe…

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