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Article
Critical analysis of antibacterial agents in clinical development
The antibacterial agents currently in clinical development are predominantly derivatives of well-established antibiotic classes and were selected to address the class-specific resistance mechanisms and determi...
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Article
Author Correction: Interplay between β-lactamases and new β-lactamase inhibitors
An amendment to this paper has been published and can be accessed via a link at the top of the paper.
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Article
Publisher Correction: Interplay between β-lactamases and new β-lactamase inhibitors
In figure 1 of the above article, the structure of ETX2514 was missing a double bond and methyl group. This has now been corrected in the PDF and online. The publisher apologizes to the authors and to the read...
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Article
Interplay between β-lactamases and new β-lactamase inhibitors
Resistance to β-lactam antibiotics in Gram-negative bacteria is commonly associated with production of β-lactamases, including extended-spectrum β-lactamases (ESBLs) and carbapenemases belonging to different m...
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Chapter
Synergistic Antibiotic Combinations
Synergy between antibiotics is a strictly defined microbiological phenomenon, requiring two bioactive agents to exhibit enhanced bacterial killing when the two are combined. Because of increasing antibiotic re...
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Article
What we may expect from novel antibacterial agents in the pipeline with respect to resistance and pharmacodynamic principles
There are some 43 small molecules in the antibiotic development pipeline from late preclinical stage (7 compounds) through Phase 1 (11 molecules), Phase 2 (13 molecules) to Phase 3 (12 molecules). The majority...
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Article
In vitro susceptibility of β-lactamase-producing carbapenem-resistant Enterobacteriaceae (CRE) to eravacycline
Eravacycline is a novel, fully synthetic fluorocycline antibiotic of the tetracycline class being developed for the treatment of complicated urinary tract infections and complicated intra-abdominal infections....
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Article
Synergistic MRSA combinations
Meropenem/piperacillin/tazobactam is a triple β-lactam combination that kills MRSA in vitro and in a mouse model through a novel synergistic mechanism of action. Similar activity for other carbapenem/β-lactam com...
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Article
The ABCD’s of β-lactamase nomenclature
β-Lactamases can be named on the basis of molecular characteristics or functional properties. Molecular classes A, B, C, and D define an enzyme according to amino acid sequence and conserved motifs. Functional...
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Chapter
Evolution of β-Lactamases: Past, Present, and Future
β-Lactamases represent some of the most widely studied examples of protein evolution, with mutations and new enzyme forms closely related to the introduction and use of novel β-lactam antibiotics. Early antibi...
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Article
Tackling antibiotic resistance
The increasing levels of antibiotic resistance observed in clinical isolates, coupled with a lack of new drugs coming through the development pipeline, make the problem of antibiotic resistance a global crisis...
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Article
Bench-to-bedside review: The role of β-lactamases in antibiotic-resistant Gram-negative infections
Multidrug resistance has been increasing among Gram-negative bacteria and is strongly associated with the production of both chromosomal- and plasmid-encoded β-lactamases, whose number now exceeds 890. Many of...
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Article
Inhibition of metallo-β-lactamases by pyridine monothiocarboxylic acid analogs
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Chapter
The Importance of β-Lactamases to the Development of New β-Lactams
β-Lactams are considered to be among the safest, most efficacious, and most widely prescribed antibiotics for the treatment of bacterial infections. Their therapeutic use began with the introduction of benzylp...
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Article
Preparation of Erythromycin Analogs Having Functional Groups at C-15
Chemobiosynthesis has been used to prepare analogs of erythromycins having unique functional groups at the 15-position. Using diketide thioester feeding to genetically engineered Streptomyces coelicolor, analogs ...
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Article
Fluoroquinolone-modifying enzyme: a new adaptation of a common aminoglycoside acetyltransferase
Antimicrobial-modifying resistance enzymes have traditionally been class specific, having coevolved with the antibiotics they inactivate. Fluoroquinolones, antimicrobial agents used extensively in medicine and...
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Article
15-Amido Erythromycins: Synthesis and in Vitro Activity of a New Class of Macrolide Antibiotics
An array of 15-amido substituted erythromycin A compounds was synthesized using a chemobiosynthesis approach. It was found that while the in vitro antibacterial activities of aryl amides were inferior to erythrom...
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Chapter
The Genomics Approach: Is it Really the Solution?
Antimicrobial drug discovery has undergone major changes over the past 25 years, with a shift in emphasis from natural product screening for whole cell inhibitory activity to biochemical approaches. However, a...
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Chapter
How β-Lactamases Have Driven Pharmaceutical Drug Discovery
Although antibiotic resistance has only recently become a recognized topic for the popular press, resistance has been the major stimulus for the pharmaceutical development of novel β-lactam antibiotics. Benzyl...
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Article
Activity of sulfa drugs and dihydrofolate reductase inhibitors againstCandida albicans
Growth ofCandida albicans can be inhibited by sulfa drugs which prevent biosynthesis of folic acid. The dihydrofolate reductase (E.C. 1.5.1.3) inhibitors aminopterin and methotrexate also exhibit anticandidal act...
