A γ-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli.
Animals
Anti-Bacterial Agents
/ chemical synthesis
Bacterial Proteins
/ antagonists & inhibitors
Binding Sites
Catalytic Domain
Crystallography, X-Ray
Drug Resistance, Multiple, Bacterial
/ drug effects
Gram-Negative Bacteria
/ drug effects
Half-Life
Lactams
/ chemistry
Mice
Microbial Sensitivity Tests
Molecular Docking Simulation
Penicillin-Binding Proteins
/ antagonists & inhibitors
Pseudomonas aeruginosa
/ metabolism
Siderophores
/ chemistry
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
11 06 2020
11 06 2020
Historique:
pubmed:
19
5
2020
medline:
13
11
2020
entrez:
19
5
2020
Statut:
ppublish
Résumé
Treatment of multidrug-resistant Gram-negative bacterial pathogens represents a critical clinical need. Here, we report a novel γ-lactam pyrazolidinone that targets penicillin-binding proteins (PBPs) and incorporates a siderophore moiety to facilitate uptake into the periplasm. The MIC values of γ-lactam YU253434,
Identifiants
pubmed: 32420736
doi: 10.1021/acs.jmedchem.0c00255
pmc: PMC7590959
mid: NIHMS1635085
doi:
Substances chimiques
Anti-Bacterial Agents
0
Bacterial Proteins
0
Lactams
0
Penicillin-Binding Proteins
0
Siderophores
0
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
5990-6002Subventions
Organisme : NIAID NIH HHS
ID : R01 AI100560
Pays : United States
Organisme : NIAID NIH HHS
ID : UM1 AI104681
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI072219
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI063517
Pays : United States
Organisme : NIAID NIH HHS
ID : K08 AI112506
Pays : United States
Organisme : BLRD VA
ID : I01 BX001974
Pays : United States
Organisme : BLRD VA
ID : I01 BX002872
Pays : United States
Organisme : NIGMS NIH HHS
ID : P41 GM103393
Pays : United States
Organisme : NCATS NIH HHS
ID : UL1 TR001863
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI090155
Pays : United States
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