Novel inhibitors of leukocyte transendothelial migration.

Tamar Getter,Raanan Margalit,Shirin Kahremany,Laura Levy,Eliav Blum,Netaly Khazanov,Nimrod Y Keshet-Levy,Tigist Y Tamir,M Ben Major,Ron Lahav, Sofia Zilber,Hanoch Senderowitz,Paul Bradfield,Beat A Imhof,Evgenia Alpert,Arie Gruzman

Bioorganic Chemistry（2019）

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摘要

•Discovery of a potent inhibitor of leucocyte transmigration.•The lead compound was not toxic in GLP toxicity experiments during 28 days of daily administration.•The lead compound was active in four in vivo inflammation/autoimmunity models.•The compound might inhibit the active form of PECAM1.

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关键词

Leukocyte transmigration,Trioxotetrahydropyrimidin derivatives,Multiple sclerosis,IBD/Crohn’s disease,Arthritis,Fatty liver

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