FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2039945407> ?p ?o ?g. }

• W2039945407 endingPage "523" @default.
• W2039945407 startingPage "503" @default.
• W2039945407 abstract "Different inflammatory diseases and allergic reactions are mediated by leukotrienes, which arise from the oxygenation of arachidonic acid catalyzed by 5-lipoxygenase (5-LO). One promising approach for an effective anti-leukotriene therapy is the inhibition of this key enzyme. This study presents the synthesis and development of a potent and direct 5-LO inhibitor based on the well characterized 5-benzylidene-2-phenylthiazolone C06, whose further pharmacological investigation was precluded due to its low solubility. Through optimization of C06, evaluation of structure–activity relationships including profound assessment of the thiazolone core and consideration of the solubility, the 5-benzyl-2-phenyl-4-hydroxythiazoles represented by 46 (ST-1829, 5-(4-chlorobenzyl)-2-p-tolylthiazol-4-ol) were developed. Compound 46 showed an improved 5-LO inhibitory activity in cell-based (IC50 values 0.14 μM) and cell-free assays (IC50 values 0.03 μM) as well as a prominent enhanced solubility. Furthermore, it kept its promising inhibitory potency in the presence of blood serum, excluding excessive binding to serum proteins. These facts combined with the non-cytotoxic profile mark a major step towards an effective anti-inflammatory therapy." @default.
• W2039945407 created "2016-06-24" @default.
• W2039945407 creator A5013929793 @default.
• W2039945407 creator A5016614839 @default.
• W2039945407 creator A5019047498 @default.
• W2039945407 creator A5066479964 @default.
• W2039945407 creator A5082078699 @default.
• W2039945407 date "2015-01-01" @default.
• W2039945407 modified "2023-09-24" @default.
• W2039945407 title "Development and evaluation of ST-1829 based on 5-benzylidene-2-phenylthiazolones as promising agent for anti-leukotriene therapy" @default.
• W2039945407 cites W1504792186 @default.
• W2039945407 cites W1544399526 @default.
• W2039945407 cites W1969480346 @default.
• W2039945407 cites W1971202181 @default.
• W2039945407 cites W1973696157 @default.
• W2039945407 cites W1976217481 @default.
• W2039945407 cites W1976419604 @default.
• W2039945407 cites W1981324981 @default.
• W2039945407 cites W1982346259 @default.
• W2039945407 cites W2005823826 @default.
• W2039945407 cites W2015478649 @default.
• W2039945407 cites W2020646338 @default.
• W2039945407 cites W2022097029 @default.
• W2039945407 cites W2023213942 @default.
• W2039945407 cites W2024176341 @default.
• W2039945407 cites W2025563699 @default.
• W2039945407 cites W2027756094 @default.
• W2039945407 cites W2038575244 @default.
• W2039945407 cites W2042950718 @default.
• W2039945407 cites W2043509228 @default.
• W2039945407 cites W2043571667 @default.
• W2039945407 cites W2045600889 @default.
• W2039945407 cites W2049796670 @default.
• W2039945407 cites W2051670789 @default.
• W2039945407 cites W2058521664 @default.
• W2039945407 cites W2066313752 @default.
• W2039945407 cites W2069340847 @default.
• W2039945407 cites W2082599261 @default.
• W2039945407 cites W2089790471 @default.
• W2039945407 cites W2109870158 @default.
• W2039945407 cites W2121737195 @default.
• W2039945407 cites W2129280925 @default.
• W2039945407 cites W2133078504 @default.
• W2039945407 cites W2135431194 @default.
• W2039945407 cites W2137673461 @default.
• W2039945407 cites W2138972132 @default.
• W2039945407 cites W2319885156 @default.
• W2039945407 cites W2626246102 @default.
• W2039945407 cites W2949060398 @default.
• W2039945407 cites W2950180967 @default.
• W2039945407 cites W2950905731 @default.
• W2039945407 cites W2952635004 @default.
• W2039945407 cites W4237270851 @default.
• W2039945407 doi "https://doi.org/10.1016/j.ejmech.2014.10.054" @default.
• W2039945407 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25462262" @default.
• W2039945407 hasPublicationYear "2015" @default.
• W2039945407 type Work @default.
• W2039945407 sameAs 2039945407 @default.
• W2039945407 citedByCount "12" @default.
• W2039945407 countsByYear W20399454072015 @default.
• W2039945407 countsByYear W20399454072016 @default.
• W2039945407 countsByYear W20399454072017 @default.
• W2039945407 countsByYear W20399454072018 @default.
• W2039945407 countsByYear W20399454072019 @default.
• W2039945407 countsByYear W20399454072022 @default.
• W2039945407 countsByYear W20399454072023 @default.
• W2039945407 crossrefType "journal-article" @default.
• W2039945407 hasAuthorship W2039945407A5013929793 @default.
• W2039945407 hasAuthorship W2039945407A5016614839 @default.
• W2039945407 hasAuthorship W2039945407A5019047498 @default.
• W2039945407 hasAuthorship W2039945407A5066479964 @default.
• W2039945407 hasAuthorship W2039945407A5082078699 @default.
• W2039945407 hasConcept C109316439 @default.
• W2039945407 hasConcept C155574463 @default.
• W2039945407 hasConcept C178790620 @default.
• W2039945407 hasConcept C181199279 @default.
• W2039945407 hasConcept C185592680 @default.
• W2039945407 hasConcept C202751555 @default.
• W2039945407 hasConcept C203014093 @default.
• W2039945407 hasConcept C21951064 @default.
• W2039945407 hasConcept C2776042228 @default.
• W2039945407 hasConcept C2776452501 @default.
• W2039945407 hasConcept C2777752497 @default.
• W2039945407 hasConcept C2778078955 @default.
• W2039945407 hasConcept C2779543280 @default.
• W2039945407 hasConcept C2780857362 @default.
• W2039945407 hasConcept C2781370401 @default.
• W2039945407 hasConcept C55493867 @default.
• W2039945407 hasConcept C57992300 @default.
• W2039945407 hasConcept C71240020 @default.
• W2039945407 hasConcept C71924100 @default.
• W2039945407 hasConcept C86803240 @default.
• W2039945407 hasConcept C90342290 @default.
• W2039945407 hasConcept C98274493 @default.
• W2039945407 hasConceptScore W2039945407C109316439 @default.
• W2039945407 hasConceptScore W2039945407C155574463 @default.
• W2039945407 hasConceptScore W2039945407C178790620 @default.
• W2039945407 hasConceptScore W2039945407C181199279 @default.

• next