1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
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DOI：
10.1021/jm025522z
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发表时间：
2002-05
影响因子：
7.3
通讯作者：
E. B. Villhauer;J. Brinkman;Goli B Naderi;B. Dunning;B. L. Mangold;M. Mone;M. E. Russell;S. Weldon;T. Hughes
中科院分区：
文献类型：
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作者：
E. B. Villhauer;J. Brinkman;Goli B Naderi;B. Dunning;B. L. Mangold;M. Mone;M. E. Russell;S. Weldon;T. Hughes
二肽基肽酶IV（DPP-IV）抑制有可能成为2型糖尿病的一种有价值的治疗方法。我们报告的第一个使用固相合成中发现的一个新的DPP-IV抑制剂类和溶液相合成，是实用的多公斤级。一种化合物NVP-DPP 728（2）被认为是一种有效的、选择性的短效DPP-IV抑制剂，具有优异的口服生物利用度和有效的抗高血糖活性。
Dipeptidyl peptidase IV (DPP-IV) inhibition has the potential to become a valuable therapy for type 2 diabetes. We report the first use of solid-phase synthesis in the discovery of a new DPP-IV inhibitor class and a solution-phase synthesis that is practical up to the multikilogram scale. One compound, NVP-DPP728 (2), is profiled as a potent, selective, and short-acting DPP-IV inhibitor that has excellent oral bioavailability and potent antihyperglycemic activity.