Matches in SemOpenAlex for { <https://semopenalex.org/work/W2046918085> ?p ?o ?g. }
Showing items 1 to 88 of
88
with 100 items per page.
- W2046918085 endingPage "234" @default.
- W2046918085 startingPage "225" @default.
- W2046918085 abstract "Thiacetazone (TAZ), one of the oldest known antituberculosis drugs, causes severe skin reactions in patients co-infected with tuberculosis and human immunodeficiency virus (HIV). KBF611 is a new fluorinated thiacetazone analogue that has shown strong antituberculosis effects. In order to provide valuable information for subsequent preclinical development, pharmacokinetics of KBF611 and its analogue (TAZ) were studied and compared in two animal species (mice and rabbits) following intravenous and oral administration, and pharmacokinetic parameters were characterized. According to the calculated parameters, KBF611 showed a more favourable pharmacokinetics profile than TAZ in terms of half-life (0.89 h compared with 0.57 in mice, p < 0.05, and 2.71 compared with 0.98 in rabbits, p < 0.001) and volume of distribution (1.45 l kg(-1) compared with 0.86 l kg(-1) in mice, p < 0.05, and 1.01 l kg(-1) compared with 0.41 l kg(-1) in rabbits, p < 0.001) for tuberculosis therapy. In rabbits, the oral bioavailability of KBF611 was markedly lower than mice (39% compared with 82%), which may be attributed to a higher presystemic metabolism in rabbit liver. The results of in vivo studies on the metabolism of KBF611, supported by liquid chromatography-mass spectrometry (LC-MS) analysis, showed that the incorporation of a fluorine atom to the TAZ structure made the molecule susceptible to N-deacetylation, a pathway not seen in TAZ metabolism. In summary, KBF611 could be considered a suitable candidate for further preclinical and clinical evaluation." @default.
- W2046918085 created "2016-06-24" @default.
- W2046918085 creator A5008684643 @default.
- W2046918085 creator A5015932384 @default.
- W2046918085 creator A5028990189 @default.
- W2046918085 creator A5045847838 @default.
- W2046918085 date "2009-12-29" @default.
- W2046918085 modified "2023-09-27" @default.
- W2046918085 title "Preclinical pharmacokinetics of KBF611, a new antituberculosis agent in mice and rabbits, and comparison with thiacetazone" @default.
- W2046918085 cites W1982951681 @default.
- W2046918085 cites W1993358760 @default.
- W2046918085 cites W2015771874 @default.
- W2046918085 cites W2024031645 @default.
- W2046918085 cites W2029789274 @default.
- W2046918085 cites W2040802012 @default.
- W2046918085 cites W2043208187 @default.
- W2046918085 cites W2054665225 @default.
- W2046918085 cites W2076757941 @default.
- W2046918085 cites W2079678142 @default.
- W2046918085 cites W2113773958 @default.
- W2046918085 cites W2135681003 @default.
- W2046918085 cites W2143563812 @default.
- W2046918085 cites W2171654601 @default.
- W2046918085 cites W2502670554 @default.
- W2046918085 cites W4211104832 @default.
- W2046918085 doi "https://doi.org/10.3109/00498250903461411" @default.
- W2046918085 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20038272" @default.
- W2046918085 hasPublicationYear "2009" @default.
- W2046918085 type Work @default.
- W2046918085 sameAs 2046918085 @default.
- W2046918085 citedByCount "10" @default.
- W2046918085 countsByYear W20469180852012 @default.
- W2046918085 countsByYear W20469180852013 @default.
- W2046918085 countsByYear W20469180852014 @default.
- W2046918085 countsByYear W20469180852015 @default.
- W2046918085 countsByYear W20469180852017 @default.
- W2046918085 countsByYear W20469180852020 @default.
- W2046918085 countsByYear W20469180852021 @default.
- W2046918085 countsByYear W20469180852022 @default.
- W2046918085 crossrefType "journal-article" @default.
- W2046918085 hasAuthorship W2046918085A5008684643 @default.
- W2046918085 hasAuthorship W2046918085A5015932384 @default.
- W2046918085 hasAuthorship W2046918085A5028990189 @default.
- W2046918085 hasAuthorship W2046918085A5045847838 @default.
- W2046918085 hasConcept C112705442 @default.
- W2046918085 hasConcept C126322002 @default.
- W2046918085 hasConcept C139254425 @default.
- W2046918085 hasConcept C150903083 @default.
- W2046918085 hasConcept C181389837 @default.
- W2046918085 hasConcept C207001950 @default.
- W2046918085 hasConcept C2777056448 @default.
- W2046918085 hasConcept C62231903 @default.
- W2046918085 hasConcept C71924100 @default.
- W2046918085 hasConcept C86803240 @default.
- W2046918085 hasConcept C98274493 @default.
- W2046918085 hasConceptScore W2046918085C112705442 @default.
- W2046918085 hasConceptScore W2046918085C126322002 @default.
- W2046918085 hasConceptScore W2046918085C139254425 @default.
- W2046918085 hasConceptScore W2046918085C150903083 @default.
- W2046918085 hasConceptScore W2046918085C181389837 @default.
- W2046918085 hasConceptScore W2046918085C207001950 @default.
- W2046918085 hasConceptScore W2046918085C2777056448 @default.
- W2046918085 hasConceptScore W2046918085C62231903 @default.
- W2046918085 hasConceptScore W2046918085C71924100 @default.
- W2046918085 hasConceptScore W2046918085C86803240 @default.
- W2046918085 hasConceptScore W2046918085C98274493 @default.
- W2046918085 hasIssue "3" @default.
- W2046918085 hasLocation W20469180851 @default.
- W2046918085 hasLocation W20469180852 @default.
- W2046918085 hasOpenAccess W2046918085 @default.
- W2046918085 hasPrimaryLocation W20469180851 @default.
- W2046918085 hasRelatedWork W2005031996 @default.
- W2046918085 hasRelatedWork W2020343058 @default.
- W2046918085 hasRelatedWork W2022148560 @default.
- W2046918085 hasRelatedWork W2086460393 @default.
- W2046918085 hasRelatedWork W2160414036 @default.
- W2046918085 hasRelatedWork W2317627837 @default.
- W2046918085 hasRelatedWork W2379311614 @default.
- W2046918085 hasRelatedWork W2414263157 @default.
- W2046918085 hasRelatedWork W2753834235 @default.
- W2046918085 hasRelatedWork W4252988432 @default.
- W2046918085 hasVolume "40" @default.
- W2046918085 isParatext "false" @default.
- W2046918085 isRetracted "false" @default.
- W2046918085 magId "2046918085" @default.
- W2046918085 workType "article" @default.