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

被引：79

作者：

Kato, Noriyasu ^{[1
]}

Oka, Mitsuru ^{[1
]}

Murase, Takayo ^{[1
]}

Yoshida, Masahiro ^{[2
]}

Sakairi, Masao ^{[1
]}

Yamashita, Satoko ^{[1
]}

Yasuda, Yoshika ^{[1
]}

Yoshikawa, Aya ^{[2
]}

Hayashi, Yuuji ^{[1
]}

Makino, Mitsuhiro ^{[1
]}

Takeda, Motohiro ^{[1
]}

Mirensha, Yakufu ^{[3
]}

Kakigami, Takuji ^{[2
]}

机构：

[1] Sanwa Kagaku Kenkyusho Co Ltd, Cent Res Lab, Inabe City, Mie 5110406, Japan

[2] Sanwa Kagaku Kenkyusho Co Ltd, Higashi Ku, Nagoya, Aichi 4618631, Japan

[3] Xinjiang Med Univ, Urumqi 830011, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 23期

关键词：

Dipeptidyl peptidase IV; DPP-IV inhibitor; Pyrazolo[1,5-a]pyrimidine; Anagliptin; Glucagon-like peptide-1; Type 2 diabetes mellitus; CLINICAL-PRACTICE; TYPE-2; SITAGLIPTIN; GLUCAGON; SAXAGLIPTIN; PHYSIOLOGY; ALOGLIPTIN; INCRETIN; THERAPY; DRUG;

D O I：

10.1016/j.bmc.2011.09.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7221 / 7227

页数：7

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