2. Academic Validation
  3. 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

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

  • Bioorg Med Chem. 2011 Dec 1;19(23):7221-7. doi: 10.1016/j.bmc.2011.09.043.
Noriyasu Kato 1,  Mitsuru Oka,  Takayo Murase,  Masahiro Yoshida,  Masao Sakairi,  Satoko Yamashita,  Yoshika Yasuda,  Aya Yoshikawa,  Yuuji Hayashi,  Mitsuhiro Makino,  Motohiro Takeda,  Yakufu Mirensha,  Takuji Kakigami
Affiliations

Affiliation

  • 1 Central Research Laboratory, Sanwa Kagaku Kenkyusho, Co. Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan. [email protected]
PMID: 22019046 DOI: 10.1016/j.bmc.2011.09.043
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.

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