FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2004359661> ?p ?o ?g. }

• W2004359661 endingPage "1438" @default.
• W2004359661 startingPage "1428" @default.
• W2004359661 abstract "The synthesis and CysLT1 receptor affinities of a new series of highly rigid 3'- and 4'-(2-quinolinylmethoxy)- or 3'- and 4'-[2-(2-quinolinyl)ethenyl]-substituted, 6-, 7-, or 8-carboxylated flavones are described. CysLT1 receptor affinities of the flavones (down to 11 nM) were determined by their ability to displace [3H]LTD4 from its receptor in guinea pig lung membranes. Structure-affinity relationship studies showed that the relative positions of the carboxylic acid and the quinoline moiety were critical for CysLT1 affinities. While the carboxyl is optimal in the 8 position but tolerated in the 6 position, only the 6- and not the 8-tetrazole has significant activity. The quinoline moiety may be connected to the flavone skeleton by an ethenyl or a methoxy linker, but the substitution position is important for high affinity, especially in the 6-carboxylated flavones. 4'-Substituted 6-carboxyflavones are essentially inactive, whereas the 3'-substituted analogues have submicromolar CysLT1 affinity. Replacement of the quinoline by other heteroaromates generally leads to decreased affinities, with the phenyl and naphthyl analogues displaying only little or no affinity, while the 7-chloroquinoline analogue is comparable in activity to the quinoline. Flavones having CysLT1 receptor affinities of 10-30 nM were selected for determination of their inhibitory effects on the LTD4-induced contraction of guinea pig ileum in vitro. The IC50 values ranged between 15 and 100 nM. Compound 5d (8-carboxy-6-chloro-3'-(2-quinolinylmethoxy)flavone, VUF 5087) was selected for further research because of its high potency in the functional assay. This series contains the most rigid CysLT1 receptor antagonists known to date, and they are useful in the development of a CysLT1 antagonist model, which is discussed in the companion paper." @default.
• W2004359661 created "2016-06-24" @default.
• W2004359661 creator A5021247773 @default.
• W2004359661 creator A5036965031 @default.
• W2004359661 creator A5038155467 @default.
• W2004359661 creator A5048022065 @default.
• W2004359661 creator A5052558608 @default.
• W2004359661 creator A5079952042 @default.
• W2004359661 creator A5081426174 @default.
• W2004359661 date "1998-04-01" @default.
• W2004359661 modified "2023-09-29" @default.
• W2004359661 title "Synthesis and Structure−Activity Relationships of Carboxyflavones as Structurally Rigid <i>CysLT</i><i>₁</i> (LTD₄) Receptor Antagonists" @default.
• W2004359661 cites W1520307434 @default.
• W2004359661 cites W1973679985 @default.
• W2004359661 cites W1976554063 @default.
• W2004359661 cites W1992571653 @default.
• W2004359661 cites W1996425731 @default.
• W2004359661 cites W1999977880 @default.
• W2004359661 cites W2004351423 @default.
• W2004359661 cites W2007207481 @default.
• W2004359661 cites W2014677805 @default.
• W2004359661 cites W2014982517 @default.
• W2004359661 cites W2017358854 @default.
• W2004359661 cites W2029697811 @default.
• W2004359661 cites W2044927863 @default.
• W2004359661 cites W2050444360 @default.
• W2004359661 cites W2059903613 @default.
• W2004359661 cites W2072506509 @default.
• W2004359661 cites W2072568796 @default.
• W2004359661 cites W2074633647 @default.
• W2004359661 cites W2075247609 @default.
• W2004359661 cites W2080663864 @default.
• W2004359661 cites W2086752638 @default.
• W2004359661 cites W2089011069 @default.
• W2004359661 cites W2122329227 @default.
• W2004359661 cites W2399190690 @default.
• W2004359661 cites W4213025950 @default.
• W2004359661 cites W4237326913 @default.
• W2004359661 cites W4241161331 @default.
• W2004359661 cites W4323915196 @default.
• W2004359661 doi "https://doi.org/10.1021/jm970179x" @default.
• W2004359661 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9554876" @default.
• W2004359661 hasPublicationYear "1998" @default.
• W2004359661 type Work @default.
• W2004359661 sameAs 2004359661 @default.
• W2004359661 citedByCount "38" @default.
• W2004359661 countsByYear W20043596612012 @default.
• W2004359661 countsByYear W20043596612013 @default.
• W2004359661 countsByYear W20043596612014 @default.
• W2004359661 countsByYear W20043596612015 @default.
• W2004359661 countsByYear W20043596612020 @default.
• W2004359661 countsByYear W20043596612021 @default.
• W2004359661 countsByYear W20043596612022 @default.
• W2004359661 countsByYear W20043596612023 @default.
• W2004359661 crossrefType "journal-article" @default.
• W2004359661 hasAuthorship W2004359661A5021247773 @default.
• W2004359661 hasAuthorship W2004359661A5036965031 @default.
• W2004359661 hasAuthorship W2004359661A5038155467 @default.
• W2004359661 hasAuthorship W2004359661A5048022065 @default.
• W2004359661 hasAuthorship W2004359661A5052558608 @default.
• W2004359661 hasAuthorship W2004359661A5079952042 @default.
• W2004359661 hasAuthorship W2004359661A5081426174 @default.
• W2004359661 hasConcept C111919701 @default.
• W2004359661 hasConcept C170493617 @default.
• W2004359661 hasConcept C178790620 @default.
• W2004359661 hasConcept C185592680 @default.
• W2004359661 hasConcept C193042331 @default.
• W2004359661 hasConcept C202751555 @default.
• W2004359661 hasConcept C2776292868 @default.
• W2004359661 hasConcept C2776309666 @default.
• W2004359661 hasConcept C2776568683 @default.
• W2004359661 hasConcept C2778938600 @default.
• W2004359661 hasConcept C2780283098 @default.
• W2004359661 hasConcept C2780557392 @default.
• W2004359661 hasConcept C2780827033 @default.
• W2004359661 hasConcept C41008148 @default.
• W2004359661 hasConcept C43617362 @default.
• W2004359661 hasConcept C55493867 @default.
• W2004359661 hasConcept C71240020 @default.
• W2004359661 hasConceptScore W2004359661C111919701 @default.
• W2004359661 hasConceptScore W2004359661C170493617 @default.
• W2004359661 hasConceptScore W2004359661C178790620 @default.
• W2004359661 hasConceptScore W2004359661C185592680 @default.
• W2004359661 hasConceptScore W2004359661C193042331 @default.
• W2004359661 hasConceptScore W2004359661C202751555 @default.
• W2004359661 hasConceptScore W2004359661C2776292868 @default.
• W2004359661 hasConceptScore W2004359661C2776309666 @default.
• W2004359661 hasConceptScore W2004359661C2776568683 @default.
• W2004359661 hasConceptScore W2004359661C2778938600 @default.
• W2004359661 hasConceptScore W2004359661C2780283098 @default.
• W2004359661 hasConceptScore W2004359661C2780557392 @default.
• W2004359661 hasConceptScore W2004359661C2780827033 @default.
• W2004359661 hasConceptScore W2004359661C41008148 @default.
• W2004359661 hasConceptScore W2004359661C43617362 @default.
• W2004359661 hasConceptScore W2004359661C55493867 @default.
• W2004359661 hasConceptScore W2004359661C71240020 @default.
• W2004359661 hasIssue "9" @default.
• W2004359661 hasLocation W20043596611 @default.

• next