FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3012208243> ?p ?o ?g. }

• W3012208243 endingPage "2195" @default.
• W3012208243 startingPage "2187" @default.
• W3012208243 abstract "The conjugation of organometallic groups to current β-lactam antibiotics is a field of increasing study due to the ability of certain organometallic groups to enhance the antibiotic potency of these drugs. Herein, we report the antibacterial properties of two metallocenyl (ferrocenyl and ruthenocenyl) 7-aminocephalosporanic acid (7-ACA) antibiotic conjugates. Continuing a trend we found in our previous studies, the ruthenocenyl conjugate showed greater antibacterial activity than its ferrocenyl counterpart. Compared with the previously published 7-aminodesacetoxycephalosporanic acid (7-ADCA) conjugates, the 3-acetyloxymethyl group significantly improved the compounds’ activity. Furthermore, the Rc-7-ACA compound was more active against clinical Staphylococcus aureus isolates than the ampicillin reference. Noticeably, neither of the two new compounds showed an undesirable toxic effect in HeLa and L929 cells at the concentrations at which they displayed strong antibacterial effects. The antibacterial activity of the two metallocenyl 7-ACA derivatives was further confirmed by scanning electron microscopy (SEM). SEM micrographs showed that bacteria treated with metallocenyl 7-ACA derivatives feature cell wall damage and morphology changes. Using a CTX-M-14 β-lactamase competition assay based on nitrocefin hydrolysis, we showed that the Rc-7-ACA bound more favorably to CTX-M-14 than its ferrocenyl counterpart, again confirming the superiority of the ruthenocenyl moiety over the ferrocenyl one in interacting with proteins. We also report a 1.47 Å resolution crystal structure of Rc-7-ACA in complex with the CTX-M-14 E166A mutant, an enzyme sharing a similar active site configuration with penicillin-binding proteins, the molecular target of β-lactam antibiotics. These results strengthen the case for the antibacterial utility of the Rc and Fc groups." @default.
• W3012208243 created "2020-03-23" @default.
• W3012208243 creator A5004601665 @default.
• W3012208243 creator A5015251733 @default.
• W3012208243 creator A5027484410 @default.
• W3012208243 creator A5036505629 @default.
• W3012208243 creator A5039276278 @default.
• W3012208243 creator A5052676364 @default.
• W3012208243 creator A5054501436 @default.
• W3012208243 creator A5054582006 @default.
• W3012208243 creator A5059527814 @default.
• W3012208243 date "2020-04-16" @default.
• W3012208243 modified "2023-10-17" @default.
• W3012208243 title "Metallocenyl 7‐ACA Conjugates: Antibacterial Activity Studies and Atomic‐Resolution X‐ray Crystal Structure with CTX‐M β‐Lactamase" @default.
• W3012208243 cites W1178498256 @default.
• W3012208243 cites W1539796472 @default.
• W3012208243 cites W1833111122 @default.
• W3012208243 cites W190540197 @default.
• W3012208243 cites W1971106038 @default.
• W3012208243 cites W1994144563 @default.
• W3012208243 cites W2001641653 @default.
• W3012208243 cites W2005372486 @default.
• W3012208243 cites W2011679824 @default.
• W3012208243 cites W2012485659 @default.
• W3012208243 cites W2013935350 @default.
• W3012208243 cites W2016567759 @default.
• W3012208243 cites W2017356685 @default.
• W3012208243 cites W2021541661 @default.
• W3012208243 cites W2050329917 @default.
• W3012208243 cites W2064123882 @default.
• W3012208243 cites W2065078821 @default.
• W3012208243 cites W2071826282 @default.
• W3012208243 cites W2080774443 @default.
• W3012208243 cites W2081139391 @default.
• W3012208243 cites W2083168864 @default.
• W3012208243 cites W2087485637 @default.
• W3012208243 cites W2095670129 @default.
• W3012208243 cites W2099460679 @default.
• W3012208243 cites W2101444285 @default.
• W3012208243 cites W2109161099 @default.
• W3012208243 cites W2135704919 @default.
• W3012208243 cites W2143267419 @default.
• W3012208243 cites W2144081223 @default.
• W3012208243 cites W2149940840 @default.
• W3012208243 cites W2151860543 @default.
• W3012208243 cites W2154191535 @default.
• W3012208243 cites W2183569749 @default.
• W3012208243 cites W2262860928 @default.
• W3012208243 cites W2274639989 @default.
• W3012208243 cites W2309902395 @default.
• W3012208243 cites W2334576785 @default.
• W3012208243 cites W2484912239 @default.
• W3012208243 cites W2512851977 @default.
• W3012208243 cites W2519986266 @default.
• W3012208243 cites W2522699308 @default.
• W3012208243 cites W2526296695 @default.
• W3012208243 cites W2550123061 @default.
• W3012208243 cites W2584228196 @default.
• W3012208243 cites W2590625301 @default.
• W3012208243 cites W2614729403 @default.
• W3012208243 cites W2725529853 @default.
• W3012208243 cites W2751848980 @default.
• W3012208243 cites W2758440816 @default.
• W3012208243 cites W2767585537 @default.
• W3012208243 cites W2770473333 @default.
• W3012208243 cites W2781455581 @default.
• W3012208243 cites W2785900358 @default.
• W3012208243 cites W2787270596 @default.
• W3012208243 cites W2801649796 @default.
• W3012208243 cites W2902408508 @default.
• W3012208243 cites W2903051221 @default.
• W3012208243 cites W2914372986 @default.
• W3012208243 cites W2927861540 @default.
• W3012208243 cites W2955469527 @default.
• W3012208243 cites W2974843680 @default.
• W3012208243 cites W2996530972 @default.
• W3012208243 doi "https://doi.org/10.1002/cbic.202000054" @default.
• W3012208243 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32182393" @default.
• W3012208243 hasPublicationYear "2020" @default.
• W3012208243 type Work @default.
• W3012208243 sameAs 3012208243 @default.
• W3012208243 citedByCount "8" @default.
• W3012208243 countsByYear W30122082432021 @default.
• W3012208243 countsByYear W30122082432022 @default.
• W3012208243 countsByYear W30122082432023 @default.
• W3012208243 crossrefType "journal-article" @default.
• W3012208243 hasAuthorship W3012208243A5004601665 @default.
• W3012208243 hasAuthorship W3012208243A5015251733 @default.
• W3012208243 hasAuthorship W3012208243A5027484410 @default.
• W3012208243 hasAuthorship W3012208243A5036505629 @default.
• W3012208243 hasAuthorship W3012208243A5039276278 @default.
• W3012208243 hasAuthorship W3012208243A5052676364 @default.
• W3012208243 hasAuthorship W3012208243A5054501436 @default.
• W3012208243 hasAuthorship W3012208243A5054582006 @default.
• W3012208243 hasAuthorship W3012208243A5059527814 @default.
• W3012208243 hasConcept C104317684 @default.
• W3012208243 hasConcept C134306372 @default.
• W3012208243 hasConcept C185592680 @default.

• next