N-[2-({2-[(2S)-2-氰基吡咯烷-1-基]-2-氧代乙基}氨基)-2-甲基丙基]-2-甲基吡唑并[1,5-a]嘧啶-6-甲酰胺盐酸盐（阿格列汀盐酸盐）的发现和药理学特性，作为一种有效的和选择性的 DPP-IV 抑制剂。
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.
机构信息
Central Research Laboratory, Sanwa Kagaku Kenkyusho, Co. Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan.
出版信息
Bioorg Med Chem. 2011 Dec 1;19(23):7221-7. doi: 10.1016/j.bmc.2011.09.043. Epub 2011 Oct 2.
PMID:22019046
Abstract
In the course of our program for discovery of novel DPP-IV inhibitors, a series of pyrazolo[1,5-a]pyrimidines were found to be novel DPP-IV inhibitors. We identified N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (4a) and described its pharmacological profiles.
摘要
在我们发现新型 DPP-IV 抑制剂的计划过程中，发现了一系列吡唑并[1,5-a]嘧啶类化合物是新型的 DPP-IV 抑制剂。我们鉴定了 N-[2-({2-[(2S)-2-氰基吡咯烷-1-基]-2-氧代乙基}氨基)-2-甲基丙基]-2-甲基吡唑并[1,5-a]嘧啶-6-甲酰胺盐酸盐（4a），并描述了其药理学特性。
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