Leban Johann, Kralik Martin, Mies Jan, Baumgartner Roland, Gassen Michael, Tasler Stefan
4SC AG, Am Klopferspitz 19a, 82152 Martinsried, Germany.
Bioorg Med Chem Lett. 2006 Jan 15;16(2):267-70. doi: 10.1016/j.bmcl.2005.10.011. Epub 2005 Oct 21.
A previously discovered DHODH inhibitor series was further improved by replacing the cyclopentene ring by aromatic heterocycles. Different isomers of these compounds were prepared by the directed ortho-metallation procedure. The compounds are more active than the corresponding cyclopentene analogs and show potent effects on PBMC's proliferation.
通过用芳族杂环取代环戊烯环，对先前发现的二氢乳清酸脱氢酶（DHODH）抑制剂系列进行了进一步优化。通过定向邻位金属化方法制备了这些化合物的不同异构体。这些化合物比相应的环戊烯类似物更具活性，并且对人外周血单核细胞（PBMC）的增殖显示出强效作用。
