Matches in SemOpenAlex for { <https://semopenalex.org/work/W2054588306> ?p ?o ?g. }
- W2054588306 endingPage "5654" @default.
- W2054588306 startingPage "5644" @default.
- W2054588306 abstract "Benzo[b]thiophene-2-ylboronic acid, 1, is a 27 nM inhibitor of the class C β-lactamase AmpC and potentiates the activity of β-lactam antibiotics in bacteria that express this and related enzymes. As is often true, the potency of compound 1 against the enzymes is much attenuated in cell culture against Gram negative bacteria, where the minimum inhibitor concentration of compound 1 is in the mid-micromolar range. Here, we modulated the properties of this lead to enhance its ability to cross the membrane, using a combination of X-ray crystallography, structure-based design, and application of physical models of outer membrane crossing. This strategy led us to derivatives with substantially improved permeability. Also, the greater solubility of these compounds allowed us to measure their efficacy at higher concentrations than with the lead 1, leading to higher maximum potentiation of the antibiotic effect of ceftazidime on resistant bacteria." @default.
- W2054588306 created "2016-06-24" @default.
- W2054588306 creator A5001525983 @default.
- W2054588306 creator A5001578963 @default.
- W2054588306 creator A5011656230 @default.
- W2054588306 creator A5017273808 @default.
- W2054588306 creator A5025232794 @default.
- W2054588306 creator A5043973034 @default.
- W2054588306 creator A5050306209 @default.
- W2054588306 creator A5065730439 @default.
- W2054588306 creator A5067042371 @default.
- W2054588306 creator A5086565347 @default.
- W2054588306 date "2007-10-23" @default.
- W2054588306 modified "2023-09-27" @default.
- W2054588306 title "Optimizing Cell Permeation of an Antibiotic Resistance Inhibitor for Improved Efficacy" @default.
- W2054588306 cites W1563954963 @default.
- W2054588306 cites W1571433223 @default.
- W2054588306 cites W1989169986 @default.
- W2054588306 cites W2016568950 @default.
- W2054588306 cites W2042588716 @default.
- W2054588306 cites W2045548784 @default.
- W2054588306 cites W2056538346 @default.
- W2054588306 cites W2069974506 @default.
- W2054588306 cites W2074112877 @default.
- W2054588306 cites W2080267554 @default.
- W2054588306 cites W2129825395 @default.
- W2054588306 cites W2133634779 @default.
- W2054588306 cites W2135732933 @default.
- W2054588306 cites W2135839939 @default.
- W2054588306 cites W2161236679 @default.
- W2054588306 cites W33831771 @default.
- W2054588306 cites W4316093093 @default.
- W2054588306 doi "https://doi.org/10.1021/jm070643q" @default.
- W2054588306 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17956081" @default.
- W2054588306 hasPublicationYear "2007" @default.
- W2054588306 type Work @default.
- W2054588306 sameAs 2054588306 @default.
- W2054588306 citedByCount "41" @default.
- W2054588306 countsByYear W20545883062012 @default.
- W2054588306 countsByYear W20545883062013 @default.
- W2054588306 countsByYear W20545883062014 @default.
- W2054588306 countsByYear W20545883062016 @default.
- W2054588306 countsByYear W20545883062017 @default.
- W2054588306 countsByYear W20545883062018 @default.
- W2054588306 countsByYear W20545883062019 @default.
- W2054588306 countsByYear W20545883062020 @default.
- W2054588306 countsByYear W20545883062021 @default.
- W2054588306 countsByYear W20545883062022 @default.
- W2054588306 crossrefType "journal-article" @default.
- W2054588306 hasAuthorship W2054588306A5001525983 @default.
- W2054588306 hasAuthorship W2054588306A5001578963 @default.
- W2054588306 hasAuthorship W2054588306A5011656230 @default.
- W2054588306 hasAuthorship W2054588306A5017273808 @default.
- W2054588306 hasAuthorship W2054588306A5025232794 @default.
- W2054588306 hasAuthorship W2054588306A5043973034 @default.
- W2054588306 hasAuthorship W2054588306A5050306209 @default.
- W2054588306 hasAuthorship W2054588306A5065730439 @default.
- W2054588306 hasAuthorship W2054588306A5067042371 @default.
- W2054588306 hasAuthorship W2054588306A5086565347 @default.
- W2054588306 hasConcept C104317684 @default.
- W2054588306 hasConcept C146587185 @default.
- W2054588306 hasConcept C155574463 @default.
- W2054588306 hasConcept C178790620 @default.
- W2054588306 hasConcept C181199279 @default.
- W2054588306 hasConcept C185592680 @default.
- W2054588306 hasConcept C19655278 @default.
- W2054588306 hasConcept C202751555 @default.
- W2054588306 hasConcept C21951064 @default.
- W2054588306 hasConcept C2776051709 @default.
- W2054588306 hasConcept C2776968632 @default.
- W2054588306 hasConcept C2776980637 @default.
- W2054588306 hasConcept C2777637488 @default.
- W2054588306 hasConcept C2992270614 @default.
- W2054588306 hasConcept C41625074 @default.
- W2054588306 hasConcept C4937899 @default.
- W2054588306 hasConcept C501593827 @default.
- W2054588306 hasConcept C50670333 @default.
- W2054588306 hasConcept C523546767 @default.
- W2054588306 hasConcept C54355233 @default.
- W2054588306 hasConcept C547475151 @default.
- W2054588306 hasConcept C55493867 @default.
- W2054588306 hasConcept C57992300 @default.
- W2054588306 hasConcept C86803240 @default.
- W2054588306 hasConceptScore W2054588306C104317684 @default.
- W2054588306 hasConceptScore W2054588306C146587185 @default.
- W2054588306 hasConceptScore W2054588306C155574463 @default.
- W2054588306 hasConceptScore W2054588306C178790620 @default.
- W2054588306 hasConceptScore W2054588306C181199279 @default.
- W2054588306 hasConceptScore W2054588306C185592680 @default.
- W2054588306 hasConceptScore W2054588306C19655278 @default.
- W2054588306 hasConceptScore W2054588306C202751555 @default.
- W2054588306 hasConceptScore W2054588306C21951064 @default.
- W2054588306 hasConceptScore W2054588306C2776051709 @default.
- W2054588306 hasConceptScore W2054588306C2776968632 @default.
- W2054588306 hasConceptScore W2054588306C2776980637 @default.
- W2054588306 hasConceptScore W2054588306C2777637488 @default.
- W2054588306 hasConceptScore W2054588306C2992270614 @default.
- W2054588306 hasConceptScore W2054588306C41625074 @default.