Carregant...
Fitxers
Tipus de document
ArticleVersió
Versió acceptadaData de publicació
Tots els drets reservats
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/226456
New and promising type of leukotriene B4 (LTB4) antagonists based on the 1,4-benzodioxine structure
Títol de la revista
Director/Tutor
ISSN de la revista
Títol del volum
Recurs relacionat
Resum
New leukotriene B4 (LTB4) antagonists have been synthesized that can be considered as potential anti-inflammatory drugs. Structures containing the dioxygenated nucleus of 1,4-benzodioxine constitute a potential group of leukotriene B4 (LTB4) antagonists. The objective of this study was to access efficient and selective LTB4 antagonists as a way to elucidate the role of LTB4 in inflammatory processes and therefore allow the development of new types of structures based on 1,4-benzodioxine. Forty-one new 1,4-benzodioxine molecules substituted at different positions of the heterocyclic nucleus were synthesized to determine the minimum structural requirements by studying structure-activity relationships. Eighteen of them were tested in vitro and in vivo for their anti-inflammatory activity related to the antagonist character of LTB4. Pharmacological tests have shown satisfactory in vitro activity for compounds 24b, 24c and 24e with IC50's of 288, 439, 477 nM respectively. The results of the in vivo tests, carried out with the compound that presented greater activity in the in vitro tests 24b, have shown significant anti-inflammatory properties.
Matèries (anglès)
Citació
Citació
BOUISSANE, Latifa, KHOUILI, Mostafa, COUDERT, Gérard, PUJOL DILMÉ, M. dolors, GUILLAUMET, Gérald. New and promising type of leukotriene B4 (LTB4) antagonists based on the 1,4-benzodioxine structure. _European Journal of Medicinal Chemistry_. 2023. Vol. 254, núm. 115332. [consulta: 13 de febrer de 2026]. ISSN: 0223-5234. [Disponible a: https://hdl.handle.net/2445/226456]