FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4220701135> ?p ?o ?g. }

• W4220701135 abstract "A series of hybridized pyrrolidine compounds with a 1,2,4-oxadiazole moiety were synthesized to develop effective molecules against the enzymes DNA gyrase and topoisomerase IV (Topo IV). Compounds 8-20 were developed based on a previously disclosed series of compounds from our lab, but with small structural modifications in the hopes of increasing the compounds' biological activity. In comparison to novobiocin, with IC50 = 170 nM, the findings of the DNA gyrase inhibitory assay revealed that compounds 16 and 17 were the most potent of all synthesized derivatives, with IC50 values of 180 and 210 nM, respectively. Compound 17 had the strongest inhibitory effect against Escherichia coli Topo IV of all the synthesized compounds, with an IC50 value of 13 µM, which was comparable to novobiocin (IC50 = 11 µM). Therefore, hybrids 16 and 17 appeared to be potential dual-target inhibitors. In the minimal inhibitory concentration (MIC) assays, compound 17 outperformed ciprofloxacin against E. coli, with an MIC of 55 ng/ml, compared to 60 ng/ml for ciprofloxacin. Finally, the docking study, along with the in vitro experiments, supports our promising approach to effectively develop potent leads for further optimization as dual DNA gyrase and Topo IV inhibitors." @default.
• W4220701135 created "2022-04-03" @default.
• W4220701135 creator A5024928010 @default.
• W4220701135 creator A5029079863 @default.
• W4220701135 creator A5046173113 @default.
• W4220701135 creator A5052439272 @default.
• W4220701135 creator A5057291017 @default.
• W4220701135 creator A5074564694 @default.
• W4220701135 creator A5078061801 @default.
• W4220701135 creator A5080556228 @default.
• W4220701135 date "2022-04-01" @default.
• W4220701135 modified "2023-10-05" @default.
• W4220701135 title "New 1,2,4‐oxadiazole/pyrrolidine hybrids as topoisomerase IV and DNA gyrase inhibitors with promising antibacterial activity" @default.
• W4220701135 cites W1978153110 @default.
• W4220701135 cites W1979474715 @default.
• W4220701135 cites W1980482232 @default.
• W4220701135 cites W2010463671 @default.
• W4220701135 cites W2049245087 @default.
• W4220701135 cites W2069270290 @default.
• W4220701135 cites W2093742668 @default.
• W4220701135 cites W2105668062 @default.
• W4220701135 cites W2112120587 @default.
• W4220701135 cites W2118308511 @default.
• W4220701135 cites W2134967712 @default.
• W4220701135 cites W2160816268 @default.
• W4220701135 cites W2330666750 @default.
• W4220701135 cites W2331788360 @default.
• W4220701135 cites W2333152051 @default.
• W4220701135 cites W2402480458 @default.
• W4220701135 cites W2407873914 @default.
• W4220701135 cites W2560208314 @default.
• W4220701135 cites W2564247286 @default.
• W4220701135 cites W2574997685 @default.
• W4220701135 cites W2604358515 @default.
• W4220701135 cites W2771533590 @default.
• W4220701135 cites W2798005496 @default.
• W4220701135 cites W2948648471 @default.
• W4220701135 cites W3001296178 @default.
• W4220701135 cites W3012971341 @default.
• W4220701135 cites W3024954510 @default.
• W4220701135 cites W3156588285 @default.
• W4220701135 cites W3157060449 @default.
• W4220701135 cites W3159272644 @default.
• W4220701135 cites W3195925564 @default.
• W4220701135 cites W3201605169 @default.
• W4220701135 cites W3212940260 @default.
• W4220701135 doi "https://doi.org/10.1002/ardp.202100516" @default.
• W4220701135 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35363388" @default.
• W4220701135 hasPublicationYear "2022" @default.
• W4220701135 type Work @default.
• W4220701135 citedByCount "6" @default.
• W4220701135 countsByYear W42207011352022 @default.
• W4220701135 countsByYear W42207011352023 @default.
• W4220701135 crossrefType "journal-article" @default.
• W4220701135 hasAuthorship W4220701135A5024928010 @default.
• W4220701135 hasAuthorship W4220701135A5029079863 @default.
• W4220701135 hasAuthorship W4220701135A5046173113 @default.
• W4220701135 hasAuthorship W4220701135A5052439272 @default.
• W4220701135 hasAuthorship W4220701135A5057291017 @default.
• W4220701135 hasAuthorship W4220701135A5074564694 @default.
• W4220701135 hasAuthorship W4220701135A5078061801 @default.
• W4220701135 hasAuthorship W4220701135A5080556228 @default.
• W4220701135 hasConcept C104317684 @default.
• W4220701135 hasConcept C147897179 @default.
• W4220701135 hasConcept C159110408 @default.
• W4220701135 hasConcept C167125095 @default.
• W4220701135 hasConcept C176947019 @default.
• W4220701135 hasConcept C178790620 @default.
• W4220701135 hasConcept C185592680 @default.
• W4220701135 hasConcept C202751555 @default.
• W4220701135 hasConcept C2777112418 @default.
• W4220701135 hasConcept C2777752497 @default.
• W4220701135 hasConcept C2778616834 @default.
• W4220701135 hasConcept C2779448499 @default.
• W4220701135 hasConcept C2779904463 @default.
• W4220701135 hasConcept C41685203 @default.
• W4220701135 hasConcept C501593827 @default.
• W4220701135 hasConcept C547475151 @default.
• W4220701135 hasConcept C552990157 @default.
• W4220701135 hasConcept C55493867 @default.
• W4220701135 hasConcept C71240020 @default.
• W4220701135 hasConcept C71924100 @default.
• W4220701135 hasConceptScore W4220701135C104317684 @default.
• W4220701135 hasConceptScore W4220701135C147897179 @default.
• W4220701135 hasConceptScore W4220701135C159110408 @default.
• W4220701135 hasConceptScore W4220701135C167125095 @default.
• W4220701135 hasConceptScore W4220701135C176947019 @default.
• W4220701135 hasConceptScore W4220701135C178790620 @default.
• W4220701135 hasConceptScore W4220701135C185592680 @default.
• W4220701135 hasConceptScore W4220701135C202751555 @default.
• W4220701135 hasConceptScore W4220701135C2777112418 @default.
• W4220701135 hasConceptScore W4220701135C2777752497 @default.
• W4220701135 hasConceptScore W4220701135C2778616834 @default.
• W4220701135 hasConceptScore W4220701135C2779448499 @default.
• W4220701135 hasConceptScore W4220701135C2779904463 @default.
• W4220701135 hasConceptScore W4220701135C41685203 @default.
• W4220701135 hasConceptScore W4220701135C501593827 @default.
• W4220701135 hasConceptScore W4220701135C547475151 @default.
• W4220701135 hasConceptScore W4220701135C552990157 @default.
• W4220701135 hasConceptScore W4220701135C55493867 @default.

• next