Matches in SemOpenAlex for { <https://semopenalex.org/work/W3026468320> ?p ?o ?g. }
- W3026468320 endingPage "103965" @default.
- W3026468320 startingPage "103965" @default.
- W3026468320 abstract "New Delhi Metallo-β-lactamase-1 (NDM-1), a Zn (II)-dependent enzyme, can catalyze the hydrolysis of almost all β-lactam antibiotics including carbapenems, resulting in bacterial antibiotic resistance, which threatens public health globally. Based on our finding that H2dedpa is as an efficient NDM-1 inhibitor, a series of H2dedpa derivatives was systematically prepared. These compounds exhibited significant activity against NDM-1, with IC50 values 0.06–0.94 μM. In vitro, compounds 6k and 6n could restore the activity of meropenem against Klebsiella pneumoniae, Escherichia coli and Proteus mirabilis possessing either NDM or IMP. In particular, the activity of meropenem against E. coli producing NDM-4 could be improved up to 5333 times when these two compounds were used. Time–kill cell-based assays showed that 99.9% of P. mirabilis were killed when treated with meropenem in combination with compound 6k or 6n. Furthermore, compounds 6k and 6n were nonhemolytic (HC50 > 1280 μg/mL) and showed low toxicity toward mammalian (HeLa) cells. Mechanistic studies indicated that compounds 6k and 6n inhibit NDM-1 by chelating the Zn2+ ion of the enzyme." @default.
- W3026468320 created "2020-05-29" @default.
- W3026468320 creator A5003402779 @default.
- W3026468320 creator A5010982644 @default.
- W3026468320 creator A5016301169 @default.
- W3026468320 creator A5022106036 @default.
- W3026468320 creator A5025666746 @default.
- W3026468320 creator A5027566811 @default.
- W3026468320 creator A5035526490 @default.
- W3026468320 creator A5050398295 @default.
- W3026468320 creator A5061284280 @default.
- W3026468320 creator A5075873781 @default.
- W3026468320 creator A5077154441 @default.
- W3026468320 date "2020-08-01" @default.
- W3026468320 modified "2023-10-15" @default.
- W3026468320 title "Systematic research of H2dedpa derivatives as potent inhibitors of New Delhi Metallo-β-lactamase-1" @default.
- W3026468320 cites W1895007034 @default.
- W3026468320 cites W1938922303 @default.
- W3026468320 cites W1991152587 @default.
- W3026468320 cites W2005530938 @default.
- W3026468320 cites W2010879752 @default.
- W3026468320 cites W2015813623 @default.
- W3026468320 cites W2020662495 @default.
- W3026468320 cites W2024888086 @default.
- W3026468320 cites W2031165491 @default.
- W3026468320 cites W2042686614 @default.
- W3026468320 cites W2061134507 @default.
- W3026468320 cites W2073060607 @default.
- W3026468320 cites W2073622666 @default.
- W3026468320 cites W2081183202 @default.
- W3026468320 cites W2097840737 @default.
- W3026468320 cites W2104843155 @default.
- W3026468320 cites W2107352206 @default.
- W3026468320 cites W2118700437 @default.
- W3026468320 cites W2121660668 @default.
- W3026468320 cites W2124002513 @default.
- W3026468320 cites W2167980905 @default.
- W3026468320 cites W2169152034 @default.
- W3026468320 cites W2293635874 @default.
- W3026468320 cites W2591028250 @default.
- W3026468320 cites W2607607338 @default.
- W3026468320 cites W2615090780 @default.
- W3026468320 cites W2746700384 @default.
- W3026468320 cites W2750546221 @default.
- W3026468320 cites W2765263674 @default.
- W3026468320 cites W2766678109 @default.
- W3026468320 cites W2767436702 @default.
- W3026468320 cites W2767485299 @default.
- W3026468320 cites W2768232069 @default.
- W3026468320 cites W2771929457 @default.
- W3026468320 cites W2778887365 @default.
- W3026468320 cites W2785436589 @default.
- W3026468320 cites W2804501852 @default.
- W3026468320 cites W2890305171 @default.
- W3026468320 cites W2901205823 @default.
- W3026468320 cites W2911300252 @default.
- W3026468320 cites W2912925715 @default.
- W3026468320 cites W2917452646 @default.
- W3026468320 cites W2918608884 @default.
- W3026468320 cites W2921386654 @default.
- W3026468320 cites W2964192374 @default.
- W3026468320 cites W3003419647 @default.
- W3026468320 cites W3008657815 @default.
- W3026468320 cites W3009977897 @default.
- W3026468320 cites W33593040 @default.
- W3026468320 cites W4235137937 @default.
- W3026468320 cites W4252726718 @default.
- W3026468320 doi "https://doi.org/10.1016/j.bioorg.2020.103965" @default.
- W3026468320 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32485471" @default.
- W3026468320 hasPublicationYear "2020" @default.
- W3026468320 type Work @default.
- W3026468320 sameAs 3026468320 @default.
- W3026468320 citedByCount "6" @default.
- W3026468320 countsByYear W30264683202021 @default.
- W3026468320 countsByYear W30264683202022 @default.
- W3026468320 crossrefType "journal-article" @default.
- W3026468320 hasAuthorship W3026468320A5003402779 @default.
- W3026468320 hasAuthorship W3026468320A5010982644 @default.
- W3026468320 hasAuthorship W3026468320A5016301169 @default.
- W3026468320 hasAuthorship W3026468320A5022106036 @default.
- W3026468320 hasAuthorship W3026468320A5025666746 @default.
- W3026468320 hasAuthorship W3026468320A5027566811 @default.
- W3026468320 hasAuthorship W3026468320A5035526490 @default.
- W3026468320 hasAuthorship W3026468320A5050398295 @default.
- W3026468320 hasAuthorship W3026468320A5061284280 @default.
- W3026468320 hasAuthorship W3026468320A5075873781 @default.
- W3026468320 hasAuthorship W3026468320A5077154441 @default.
- W3026468320 hasConcept C104317684 @default.
- W3026468320 hasConcept C142724271 @default.
- W3026468320 hasConcept C158739034 @default.
- W3026468320 hasConcept C181199279 @default.
- W3026468320 hasConcept C185592680 @default.
- W3026468320 hasConcept C202751555 @default.
- W3026468320 hasConcept C2777058267 @default.
- W3026468320 hasConcept C2777366897 @default.
- W3026468320 hasConcept C2778039505 @default.
- W3026468320 hasConcept C2779375183 @default.
- W3026468320 hasConcept C3020456351 @default.