强效、选择性且口服生物可利用的吡啶酮基二肽基肽酶-4抑制剂的发现。
Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.
作者信息
Xu Jinyou, Wei Lan, Mathvink Robert, Edmondson Scott D, Mastracchio Anthony, Eiermann George J, He Huaibing, Leone Joseph F, Leiting Barbara, Lyons Kathryn A, Marsilio Frank, Patel Reshma A, Petrov Aleksandr, Wu Joseph K, Thornberry Nancy A, Weber Ann E
机构信息
Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1346-9. doi: 10.1016/j.bmcl.2005.11.052. Epub 2005 Dec 5.
anti-Substituted beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound exhibited good pharmacokinetic profiles in three preclinical species.
抗取代的β-甲基苯丙氨酸衍生酰胺已被证明是有效的二肽基肽酶-IV（DPP-IV）抑制剂，对DPP8和DPP9均表现出优异的选择性。优化后的化合物在三种临床前物种中表现出良好的药代动力学特征。
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