Matches in SemOpenAlex for { <https://semopenalex.org/work/W4213230100> ?p ?o ?g. }
- W4213230100 endingPage "444" @default.
- W4213230100 startingPage "436" @default.
- W4213230100 abstract "Antibiotics with fundamentally new mechanisms of action such as the armeniaspirols, which target the ATP-dependent proteases ClpXP and ClpYQ, must be developed to combat antimicrobial resistance. While the mechanism of action of armeniaspirol against Gram-positive bacteria is understood, little is known about the structure-activity relationship for its antibiotic activity. Based on the preliminary data showing that modifications of armeniaspirol's N-methyl group increased antibiotic potency, we probed the structure-activity relationship of N-alkyl armeniaspirol derivatives. A series of focused derivatives were synthesized and evaluated for antibiotic activity against clinically relevant pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus. Replacement of the N-methyl with N-hexyl, various N-benzyl, and N-phenethyl substituents led to substantial increases in antibiotic activity and potency for inhibition of both ClpYQ and ClpXP. Docking studies identified binding models for ClpXP and ClpYQ that were consistent with the inhibition data. This work confirms the role of ClpXP and ClpYQ in the mechanism of action of armeniaspirol and provides important lead compounds for further antibiotic development." @default.
- W4213230100 created "2022-02-24" @default.
- W4213230100 creator A5001066116 @default.
- W4213230100 creator A5001601542 @default.
- W4213230100 creator A5042654016 @default.
- W4213230100 creator A5050925230 @default.
- W4213230100 creator A5052667915 @default.
- W4213230100 creator A5061174540 @default.
- W4213230100 creator A5067862836 @default.
- W4213230100 creator A5077288231 @default.
- W4213230100 creator A5079693658 @default.
- W4213230100 creator A5090735655 @default.
- W4213230100 date "2022-01-01" @default.
- W4213230100 modified "2023-10-13" @default.
- W4213230100 title "Armeniaspirol analogues with more potent Gram-positive antibiotic activity show enhanced inhibition of the ATP-dependent proteases ClpXP and ClpYQ" @default.
- W4213230100 cites W1563232489 @default.
- W4213230100 cites W1853264433 @default.
- W4213230100 cites W1970632274 @default.
- W4213230100 cites W1979973356 @default.
- W4213230100 cites W1984673823 @default.
- W4213230100 cites W1985012958 @default.
- W4213230100 cites W2014203427 @default.
- W4213230100 cites W2020930543 @default.
- W4213230100 cites W2026902916 @default.
- W4213230100 cites W2040907657 @default.
- W4213230100 cites W2049789253 @default.
- W4213230100 cites W2062408808 @default.
- W4213230100 cites W2062458432 @default.
- W4213230100 cites W2072589601 @default.
- W4213230100 cites W2077439537 @default.
- W4213230100 cites W2081746541 @default.
- W4213230100 cites W2094596231 @default.
- W4213230100 cites W2096541421 @default.
- W4213230100 cites W2118405368 @default.
- W4213230100 cites W2134967712 @default.
- W4213230100 cites W2147652807 @default.
- W4213230100 cites W2167556437 @default.
- W4213230100 cites W2169018184 @default.
- W4213230100 cites W2171378731 @default.
- W4213230100 cites W2175756712 @default.
- W4213230100 cites W2334535899 @default.
- W4213230100 cites W2414802097 @default.
- W4213230100 cites W2586452052 @default.
- W4213230100 cites W2782422728 @default.
- W4213230100 cites W2799465158 @default.
- W4213230100 cites W2884958591 @default.
- W4213230100 cites W2914276606 @default.
- W4213230100 cites W2942675709 @default.
- W4213230100 cites W2971422465 @default.
- W4213230100 cites W3045487055 @default.
- W4213230100 cites W3093136605 @default.
- W4213230100 cites W3184848011 @default.
- W4213230100 cites W4245742040 @default.
- W4213230100 doi "https://doi.org/10.1039/d1md00355k" @default.
- W4213230100 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35647545" @default.
- W4213230100 hasPublicationYear "2022" @default.
- W4213230100 type Work @default.
- W4213230100 citedByCount "2" @default.
- W4213230100 countsByYear W42132301002022 @default.
- W4213230100 countsByYear W42132301002023 @default.
- W4213230100 crossrefType "journal-article" @default.
- W4213230100 hasAuthorship W4213230100A5001066116 @default.
- W4213230100 hasAuthorship W4213230100A5001601542 @default.
- W4213230100 hasAuthorship W4213230100A5042654016 @default.
- W4213230100 hasAuthorship W4213230100A5050925230 @default.
- W4213230100 hasAuthorship W4213230100A5052667915 @default.
- W4213230100 hasAuthorship W4213230100A5061174540 @default.
- W4213230100 hasAuthorship W4213230100A5067862836 @default.
- W4213230100 hasAuthorship W4213230100A5077288231 @default.
- W4213230100 hasAuthorship W4213230100A5079693658 @default.
- W4213230100 hasAuthorship W4213230100A5090735655 @default.
- W4213230100 hasBestOaLocation W42132301002 @default.
- W4213230100 hasConcept C159110408 @default.
- W4213230100 hasConcept C181199279 @default.
- W4213230100 hasConcept C182220744 @default.
- W4213230100 hasConcept C185592680 @default.
- W4213230100 hasConcept C193042331 @default.
- W4213230100 hasConcept C202751555 @default.
- W4213230100 hasConcept C2776120743 @default.
- W4213230100 hasConcept C41685203 @default.
- W4213230100 hasConcept C4937899 @default.
- W4213230100 hasConcept C501593827 @default.
- W4213230100 hasConcept C523546767 @default.
- W4213230100 hasConcept C54355233 @default.
- W4213230100 hasConcept C55493867 @default.
- W4213230100 hasConcept C57992300 @default.
- W4213230100 hasConcept C71924100 @default.
- W4213230100 hasConcept C86803240 @default.
- W4213230100 hasConcept C89423630 @default.
- W4213230100 hasConceptScore W4213230100C159110408 @default.
- W4213230100 hasConceptScore W4213230100C181199279 @default.
- W4213230100 hasConceptScore W4213230100C182220744 @default.
- W4213230100 hasConceptScore W4213230100C185592680 @default.
- W4213230100 hasConceptScore W4213230100C193042331 @default.
- W4213230100 hasConceptScore W4213230100C202751555 @default.
- W4213230100 hasConceptScore W4213230100C2776120743 @default.
- W4213230100 hasConceptScore W4213230100C41685203 @default.
- W4213230100 hasConceptScore W4213230100C4937899 @default.