Getter, Tamar; Margalit, Raanan; Kahremany, Shirin; Levy, Laura; Blum, Eliav; Khazanov, Netaly; Keshet-Levy, Nimrod Y.; Tamir, Tigist Y.; Ben Major, M.; Lahav, Ron; Zilber, Sofia; Senderowitz, Hanoch; Bradfield, Paul; Imhof, Beat A.; Alpert, Evgenia; Gruzman, Arie published the artcile< Novel inhibitors of leukocyte transendothelial migration>, Safety of Methyl 4-(bromomethyl)-2-fluorobenzoate, the main research area is benzylidene trioxotetrahydropyrimidine preparation leukocyte transendothelial migration inhibitor docking human; Arthritis; Fatty liver; IBD/Crohn’s disease; Leukocyte transmigration; Multiple sclerosis; Trioxotetrahydropyrimidin derivatives.
In this study, based on previous trioxotetrahydropyrimidine based integrin inhibitors that suboptimally blocked leukocyte adhesion, twelve mols. with a modified scaffold were designed, synthesized, and tested in vitro for their capacity to block the transendothelial migration of immune cells. One of the mols. I, completely blocked leukocyte transendothelial migration, without any toxic effects on immune or endothelial cells (IC50 = 2.4 μM). In vivo, compound I exhibited significant therapeutic effects in inflammatory bowel disease (IBD)/Crohn’s disease, multiple sclerosis, fatty liver disease, and rheumatoid arthritis models. A detailed acute and chronic toxicity profile of the lead compound in vivo did not reveal any toxic effects. Such a type of mol. might therefore provide a unique starting point for designing a novel class of leukocyte transmigration blocking agents with broad therapeutic applications in inflammatory and auto-immune pathologies.
Bioorganic Chemistry published new progress about Anti-inflammatory agents. 85070-57-1 belongs to class bromides-buliding-blocks, and the molecular formula is C9H8BrFO2, Safety of Methyl 4-(bromomethyl)-2-fluorobenzoate.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary