Matches in SemOpenAlex for { <https://semopenalex.org/work/W1549521446> ?p ?o ?g. }
Showing items 1 to 95 of
95
with 100 items per page.
- W1549521446 endingPage "7887" @default.
- W1549521446 startingPage "7879" @default.
- W1549521446 abstract "Abstract Two novel C10-(dipeptidyl)cephalosporin esters (3-(beta-chloro-L-alanyl-beta-chloro-L-alanyloxymethyl)-7 beta-(2-thienylacetamido)-3-cephem-4-carboxylic acid (7) and sodium 3-(L-alanyl-L-alanyloxymethyl)-7 beta-(2-thienylacetamido)-3-cephem-4-carboxylate, toluene-sulfonic acid salt (18] were synthesized, and their reactions with Escherichia coli TEM beta-lactamase were examined. Kinetic parameters determined for the enzymatic reactions of 7 (Km = 0.32 mM; Vmax = 338 mumol min-1 (mg protein)-1) and of 18 (Km = 0.33 mM, Vmax = 338 mumol min-1 (mg protein)-1) demonstrate that both of the peptidyl esters are good substrates for the lactamase. In fact, the Vmax rates for 7 and 18 are each more than 4-fold greater than that obtained for cephalothin, 1 (Vmax = 78 mumol min-1 (mg protein)-1), a well characterized substrate for the lactamases. Analysis of the enzymatic reactions by high field (500 MHz) 1H NMR revealed similar patterns for fragmentation of the cephem nucleus of 1, 7, and 18. However, while hydrolysis of 1 produces acetate, cleavage of 7 and 18 releases beta Cl-LAla-beta Cl-LAla and LAla-LAla, respectively, from the dipeptidyl cephalosporin esters. Based on these findings, a strategy for co-opting the beta-lactamases of Gram-negative bacteria for delivery of bactericidal agents is described, and an explanation for the previously reported (Mobashery, S., Lerner, S.A., and Johnston, M. (1986) J. Am. Chem. Soc. 108, 1685) antibacterial activity of 7 is offered." @default.
- W1549521446 created "2016-06-24" @default.
- W1549521446 creator A5013812375 @default.
- W1549521446 creator A5069838718 @default.
- W1549521446 date "1986-06-01" @default.
- W1549521446 modified "2023-09-29" @default.
- W1549521446 title "Reactions of Escherichia coli TEM beta-lactamase with cephalothin and with C10-dipeptidyl cephalosporin esters." @default.
- W1549521446 cites W1519296568 @default.
- W1549521446 cites W152638252 @default.
- W1549521446 cites W1598457475 @default.
- W1549521446 cites W168483134 @default.
- W1549521446 cites W1775749144 @default.
- W1549521446 cites W1940914177 @default.
- W1549521446 cites W1942872363 @default.
- W1549521446 cites W1967517081 @default.
- W1549521446 cites W1969725038 @default.
- W1549521446 cites W1974178486 @default.
- W1549521446 cites W1978382870 @default.
- W1549521446 cites W1981945182 @default.
- W1549521446 cites W1990494770 @default.
- W1549521446 cites W1996825380 @default.
- W1549521446 cites W2000831821 @default.
- W1549521446 cites W2015380322 @default.
- W1549521446 cites W2015751321 @default.
- W1549521446 cites W2026368319 @default.
- W1549521446 cites W2032512166 @default.
- W1549521446 cites W2032782882 @default.
- W1549521446 cites W2035648196 @default.
- W1549521446 cites W2043014652 @default.
- W1549521446 cites W2046505487 @default.
- W1549521446 cites W2049012264 @default.
- W1549521446 cites W2075557847 @default.
- W1549521446 cites W2078302145 @default.
- W1549521446 cites W2086153842 @default.
- W1549521446 cites W2091621771 @default.
- W1549521446 cites W2112260160 @default.
- W1549521446 cites W2416364999 @default.
- W1549521446 cites W2508578651 @default.
- W1549521446 doi "https://doi.org/10.1016/s0021-9258(19)57485-3" @default.
- W1549521446 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/3519615" @default.
- W1549521446 hasPublicationYear "1986" @default.
- W1549521446 type Work @default.
- W1549521446 sameAs 1549521446 @default.
- W1549521446 citedByCount "26" @default.
- W1549521446 countsByYear W15495214462012 @default.
- W1549521446 countsByYear W15495214462014 @default.
- W1549521446 countsByYear W15495214462015 @default.
- W1549521446 countsByYear W15495214462017 @default.
- W1549521446 countsByYear W15495214462018 @default.
- W1549521446 countsByYear W15495214462019 @default.
- W1549521446 crossrefType "journal-article" @default.
- W1549521446 hasAuthorship W1549521446A5013812375 @default.
- W1549521446 hasAuthorship W1549521446A5069838718 @default.
- W1549521446 hasBestOaLocation W15495214461 @default.
- W1549521446 hasConcept C104317684 @default.
- W1549521446 hasConcept C185592680 @default.
- W1549521446 hasConcept C2781288988 @default.
- W1549521446 hasConcept C2910641391 @default.
- W1549521446 hasConcept C501593827 @default.
- W1549521446 hasConcept C547475151 @default.
- W1549521446 hasConcept C55493867 @default.
- W1549521446 hasConcept C64778159 @default.
- W1549521446 hasConcept C86803240 @default.
- W1549521446 hasConcept C89423630 @default.
- W1549521446 hasConceptScore W1549521446C104317684 @default.
- W1549521446 hasConceptScore W1549521446C185592680 @default.
- W1549521446 hasConceptScore W1549521446C2781288988 @default.
- W1549521446 hasConceptScore W1549521446C2910641391 @default.
- W1549521446 hasConceptScore W1549521446C501593827 @default.
- W1549521446 hasConceptScore W1549521446C547475151 @default.
- W1549521446 hasConceptScore W1549521446C55493867 @default.
- W1549521446 hasConceptScore W1549521446C64778159 @default.
- W1549521446 hasConceptScore W1549521446C86803240 @default.
- W1549521446 hasConceptScore W1549521446C89423630 @default.
- W1549521446 hasIssue "17" @default.
- W1549521446 hasLocation W15495214461 @default.
- W1549521446 hasOpenAccess W1549521446 @default.
- W1549521446 hasPrimaryLocation W15495214461 @default.
- W1549521446 hasRelatedWork W2068407850 @default.
- W1549521446 hasRelatedWork W2109800290 @default.
- W1549521446 hasRelatedWork W2166235873 @default.
- W1549521446 hasRelatedWork W2260529003 @default.
- W1549521446 hasRelatedWork W2298163805 @default.
- W1549521446 hasRelatedWork W2355861971 @default.
- W1549521446 hasRelatedWork W2586844040 @default.
- W1549521446 hasRelatedWork W2935619108 @default.
- W1549521446 hasRelatedWork W3092586535 @default.
- W1549521446 hasRelatedWork W3157929551 @default.
- W1549521446 hasVolume "261" @default.
- W1549521446 isParatext "false" @default.
- W1549521446 isRetracted "false" @default.
- W1549521446 magId "1549521446" @default.
- W1549521446 workType "article" @default.