Matches in SemOpenAlex for { <https://semopenalex.org/work/W4293498983> ?p ?o ?g. }
- W4293498983 endingPage "11875" @default.
- W4293498983 startingPage "11854" @default.
- W4293498983 abstract "UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC) is a promising drug target in Gram-negative bacteria. Previously, we described a correlation between the residence time of inhibitors on Pseudomonas aeruginosa LpxC (paLpxC) and the post-antibiotic effect (PAE) caused by the inhibitors on the growth of P. aeruginosa. Given that drugs with prolonged activity following compound removal may have advantages in dosing regimens, we have explored the structure-kinetic relationship for paLpxC inhibition by analogues of the pyridone methylsulfone PF5081090 (1) originally developed by Pfizer. Several analogues have longer residence times on paLpxC than 1 (41 min) including PT913, which has a residence time of 124 min. PT913 also has a PAE of 4 h, extending the original correlation observed between residence time and PAE. Collectively, the studies provide a platform for the rational modulation of paLpxC inhibitor residence time and the potential development of antibacterial agents that cause prolonged suppression of bacterial growth." @default.
- W4293498983 created "2022-08-29" @default.
- W4293498983 creator A5003151045 @default.
- W4293498983 creator A5006004732 @default.
- W4293498983 creator A5013710650 @default.
- W4293498983 creator A5013820402 @default.
- W4293498983 creator A5023214008 @default.
- W4293498983 creator A5028724991 @default.
- W4293498983 creator A5035413317 @default.
- W4293498983 creator A5049876175 @default.
- W4293498983 creator A5060185486 @default.
- W4293498983 creator A5066303259 @default.
- W4293498983 creator A5079056895 @default.
- W4293498983 date "2022-08-29" @default.
- W4293498983 modified "2023-10-18" @default.
- W4293498983 title "Structure–Kinetic Relationship Studies for the Development of Long Residence Time LpxC Inhibitors" @default.
- W4293498983 cites W1501203786 @default.
- W4293498983 cites W1557800628 @default.
- W4293498983 cites W1587498640 @default.
- W4293498983 cites W1711766424 @default.
- W4293498983 cites W1844138706 @default.
- W4293498983 cites W1975732928 @default.
- W4293498983 cites W1984678233 @default.
- W4293498983 cites W1989154905 @default.
- W4293498983 cites W1989960958 @default.
- W4293498983 cites W1996449317 @default.
- W4293498983 cites W2007805149 @default.
- W4293498983 cites W2012529917 @default.
- W4293498983 cites W2016408686 @default.
- W4293498983 cites W2035952478 @default.
- W4293498983 cites W2036828736 @default.
- W4293498983 cites W2039932426 @default.
- W4293498983 cites W2040680919 @default.
- W4293498983 cites W2054762986 @default.
- W4293498983 cites W2066253834 @default.
- W4293498983 cites W2076199143 @default.
- W4293498983 cites W2090821219 @default.
- W4293498983 cites W2094228352 @default.
- W4293498983 cites W2102150398 @default.
- W4293498983 cites W2103572010 @default.
- W4293498983 cites W2106359046 @default.
- W4293498983 cites W2109824815 @default.
- W4293498983 cites W2113038839 @default.
- W4293498983 cites W2114197590 @default.
- W4293498983 cites W2124026197 @default.
- W4293498983 cites W2132106435 @default.
- W4293498983 cites W2154714625 @default.
- W4293498983 cites W2165473666 @default.
- W4293498983 cites W2171880413 @default.
- W4293498983 cites W2180229411 @default.
- W4293498983 cites W2207535250 @default.
- W4293498983 cites W2296140671 @default.
- W4293498983 cites W2315609346 @default.
- W4293498983 cites W2402130561 @default.
- W4293498983 cites W2406190434 @default.
- W4293498983 cites W2585492454 @default.
- W4293498983 cites W2613613983 @default.
- W4293498983 cites W2620075194 @default.
- W4293498983 cites W2664285537 @default.
- W4293498983 cites W2737166234 @default.
- W4293498983 cites W2746238125 @default.
- W4293498983 cites W2868115494 @default.
- W4293498983 cites W2889833186 @default.
- W4293498983 cites W2941098942 @default.
- W4293498983 cites W2942419925 @default.
- W4293498983 cites W2946651253 @default.
- W4293498983 cites W2959149559 @default.
- W4293498983 cites W2970598936 @default.
- W4293498983 cites W2994197950 @default.
- W4293498983 cites W3004936484 @default.
- W4293498983 cites W3097315641 @default.
- W4293498983 cites W3116314579 @default.
- W4293498983 cites W3135245180 @default.
- W4293498983 cites W3190112138 @default.
- W4293498983 cites W4248335702 @default.
- W4293498983 cites W4248872320 @default.
- W4293498983 cites W4255231775 @default.
- W4293498983 cites W869085174 @default.
- W4293498983 doi "https://doi.org/10.1021/acs.jmedchem.2c00974" @default.
- W4293498983 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36037447" @default.
- W4293498983 hasPublicationYear "2022" @default.
- W4293498983 type Work @default.
- W4293498983 citedByCount "9" @default.
- W4293498983 countsByYear W42934989832023 @default.
- W4293498983 crossrefType "journal-article" @default.
- W4293498983 hasAuthorship W4293498983A5003151045 @default.
- W4293498983 hasAuthorship W4293498983A5006004732 @default.
- W4293498983 hasAuthorship W4293498983A5013710650 @default.
- W4293498983 hasAuthorship W4293498983A5013820402 @default.
- W4293498983 hasAuthorship W4293498983A5023214008 @default.
- W4293498983 hasAuthorship W4293498983A5028724991 @default.
- W4293498983 hasAuthorship W4293498983A5035413317 @default.
- W4293498983 hasAuthorship W4293498983A5049876175 @default.
- W4293498983 hasAuthorship W4293498983A5060185486 @default.
- W4293498983 hasAuthorship W4293498983A5066303259 @default.
- W4293498983 hasAuthorship W4293498983A5079056895 @default.
- W4293498983 hasConcept C127413603 @default.
- W4293498983 hasConcept C185592680 @default.