Diaryl-substituted thiosemicarbazone: A potent scaffold for the development of New Delhi metallo-β-lactamase-1 inhibitors.

Anti-Bacterial Agents / chemical synthesis Dose-Response Relationship, Drug Enzyme Inhibitors / chemical synthesis Escherichia coli / enzymology Microbial Sensitivity Tests Molecular Structure Structure-Activity Relationship Thiosemicarbazones / chemical synthesis beta-Lactamases / metabolism
Antibiotic resistance Inhibitor Metallo-β-lactamases NDM-1 Thiosemicarbazone

Journal

Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703

Informations de publication

Date de publication:
02 2021
Historique:
received: 30 09 2020
revised: 16 12 2020
accepted: 16 12 2020
pubmed: 1 1 2021
medline: 7 9 2021
entrez: 31 12 2020
Statut: ppublish

Résumé

The superbug infection caused by New Delhi metallo-β-lactamase (NDM-1) has become an emerging public health threat. Inhibition of NDM-1 has proven challenging due to its shuttling between pathogenic bacteria. A potent scaffold, diaryl-substituted thiosemicarbazone, was constructed and assayed with metallo-β-lactamases (MβLs). The obtained twenty-six molecules specifically inhibited NDM-1 with IC

Identifiants

DOI: 10.1016/j.bioorg.2020.104576 PMID: 33383326
pubmed: 33383326
pii: S0045-2068(20)31874-5
doi: 10.1016/j.bioorg.2020.104576
pii:
doi:

Substances chimiques

Anti-Bacterial Agents 0
Enzyme Inhibitors 0
Thiosemicarbazones 0
beta-Lactamases EC 3.5.2.6
beta-lactamase NDM-1 EC 3.5.2.6

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

104576

Informations de copyright

Copyright © 2020 Elsevier Inc. All rights reserved.

Auteurs

Jia-Qi Li (JQ)

Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710127, PR China.

Le-Yun Sun (LY)

Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710127, PR China.

Zhihui Jiang (Z)

Department of Pharmacy, General Hospital of Southern Theatre Command of PLA, Guangzhou 510010, PR China.

Cheng Chen (C)

Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710127, PR China.

Han Gao (H)

Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710127, PR China.

Jia-Zhu Chigan (JZ)

Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710127, PR China.

Huan-Huan Ding (HH)

Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710127, PR China.

Ke-Wu Yang (KW)

Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710127, PR China. Electronic address: kwyang@nwu.edu.cn.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Bactéries › Proteobacteria › Gammaproteobacteria › Enterobacteriaceae › Escherichia › Escherichia coli › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Composés chimiques organiques › Composés du soufre › Thiosemicarbazones › Diaryl-substituted thiosemicarbazone: A potent...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Amidohydrolases › bêta-Lactamases › Diaryl-substituted thiosemicarbazone: A potent...