强效且选择性的脯氨酸衍生二肽基肽酶IV抑制剂。
Potent and selective proline derived dipeptidyl peptidase IV inhibitors.
作者信息
Edmondson Scott D, Mastracchio Anthony, Beconi Maria, Colwell Lawrence F, Habulihaz Bahanu, He Huaibing, Kumar Sanjeev, Leiting Barbara, Lyons Kathryn A, Mao Ann, Marsilio Frank, Patel Reshma A, Wu Joseph K, Zhu Lan, Thornberry Nancy A, Weber Ann E, Parmee Emma R
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. 2004 Oct 18;14(20):5151-5. doi: 10.1016/j.bmcl.2004.07.056.
In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9 microM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date.
对默克样品库进行的内部筛选发现，脯氨酸衍生的高苯丙氨酸3是一种活性适中的二肽基肽酶-IV（DPP-IV）抑制剂（DPP-IV IC50 = 1.9微摩尔）。对3进行优化得到了化合物37，它是迄今为止发现的最有效和最具选择性的DPP-IV抑制剂之一。
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