Arzneimittel-Forschung · 2005
Pharmacological profile of 4-(2',4'-difluorobiphenyl-4-yl)-2-methylbutyric acid (deoxoflobufen).
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Bulej Petr, Kuchar Miroslav, Panajotova Vladimíra, Jegorov Alexandr
Аннотация
4-(2',4'- Difluorobiphenyl-4-yl)-2-methylbutyric acid (deoxoflobufen, VUFB 19053, CAS 847475-35-8) has been developed as a new omega-biphenyl-alkanoic acid and studied in comparison with the racemic form of 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid (flobufen, CAS 112344-52-2). The compounds were tested in a series of models including acute inflammation induced by carrageenan, adjuvant arthritis, in vitro inhibition of the leuktotriene B4 (LTB4) production, reaction of the graft versus the host (GVHR), production of specific antibodies against ovalbumin, peritoneal exudate formation induced by thioglycollate and phagocytosis of thioglycollate-stimulated mouse peritoneal macrophages. Deoxoflobufen exhibited strong anti-inflammatory, antiarthritic and immunomodulatory effects in most of the performed tests. Anti-inflammatory and antiarthritic effects are fully comparable with those of flobufen, however, the compound is less toxic and has apparently stronger immunomodulating effects.
Предметные рубрики MeSH
AnimalsAnti-Inflammatory AgentsAntibody FormationArea Under CurveArthritis, ExperimentalBiphenyl CompoundsButyratesCarrageenanCell AdhesionExudates and TransudatesFemaleGraft vs Host DiseaseHypersensitivity, DelayedInflammationLeukotriene B4MacrophagesMiceOvalbuminPeritonitisPhagocytosisPleurisyRatsStructure-Activity RelationshipThioglycolates