作为具有改善口服药代动力学性质的强效和选择性α(v)β3整合素受体拮抗剂的2,5-噻唑丁酸的合成。
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties.
作者信息
Wendt John A, Wu Hongwei, Stenmark Heather G, Boys Mark L, Downs Victoria L, Penning Thomas D, Chen Barbara B, Wang Yaping, Duffin Tiffany, Finn Mary Beth, Keene Jeffery L, Engleman V Wayne, Freeman Sandra K, Hanneke Melanie L, Shannon Kristen E, Nickols Maureen A, Steininger Christina N, Westlin Marissa, Klover Jon A, Westlin William, Nickols G Allen, Russell Mark A
机构信息
Department of Medicinal Chemistry, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
出版信息
Bioorg Med Chem Lett. 2006 Feb 15;16(4):845-9. doi: 10.1016/j.bmcl.2005.11.017. Epub 2005 Nov 21.
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin alpha(v)beta3 and show selectivity relative to the other integrins, such as alpha(IIb)beta3 and alpha(v)beta6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
我们描述了一系列含2,5 - 噻唑的化合物，它们是整合素α(v)β3的强效拮抗剂，并且相对于其他整合素，如α(IIb)β3和α(v)β6，表现出选择性。相对于其他相关杂环类似物，这些类似物被证明具有高生物利用度。
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