| Title : Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methyl pyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor - Kato_2011_Bioorg.Med.Chem_19_7221 |
| Author(s) : Kato N , Oka M , Murase T , Yoshida M , Sakairi M , Yamashita S , Yasuda Y , Yoshikawa A , Hayashi Y , Makino M , Takeda M , Mirensha Y , Kakigami T |
| Ref : Bioorganic & Medicinal Chemistry , 19 :7221 , 2011 |
|
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-methyl pyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (4a) and described its pharmacological profiles. |
| PubMedSearch : Kato_2011_Bioorg.Med.Chem_19_7221 |
| PubMedID: 22019046 |
| Inhibitor | Anagliptin |
Kato N, Oka M, Murase T, Yoshida M, Sakairi M, Yamashita S, Yasuda Y, Yoshikawa A, Hayashi Y, Makino M, Takeda M, Mirensha Y, Kakigami T (2011)
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methyl pyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor
Bioorganic & Medicinal Chemistry
19 :7221
Kato N, Oka M, Murase T, Yoshida M, Sakairi M, Yamashita S, Yasuda Y, Yoshikawa A, Hayashi Y, Makino M, Takeda M, Mirensha Y, Kakigami T (2011)
Bioorganic & Medicinal Chemistry
19 :7221