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Paper(s) concerning Anagliptin

2 reference(s) found.
Listing paper details in reverse chronological order.
We are grateful to Keith Bradnam for improvment of this script

Title: Anagliptin, a potent dipeptidyl peptidase IV inhibitor: its single-crystal structure and enzyme interactions
Watanabe YS, Yasuda Y, Kojima Y, Okada S, Motoyama T, Takahashi R, Oka M
Ref: J Enzyme Inhib Med Chem, 30:981, 2015 : PubMed
Abstract


ESTHER: Watanabe_2015_J.Enzyme.Inhib.Med.Chem_30_981
PubMedSearch: Watanabe 2015 J.Enzyme.Inhib.Med.Chem 30 981
PubMedID: 26147347
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: Anagliptin

Abstract

The single-crystal structure of anagliptin, N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methyl pyrazolo[1,5-a]pyrimidine-6-carboxamide, was determined. Two independent molecules were held together by intermolecular hydrogen bonds, and the absolute configuration of the 2-cyanopyrrolidine ring delivered from l-prolinamide was confirmed to be S. The interactions of anagliptin with DPP-4 were clarified by the co-crystal structure solved at 2.85 A resolution. Based on the structure determined by X-ray crystallography, the potency and selectivity of anagliptin were discussed, and an SAR study using anagliptin derivatives was performed.



        

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 N, Oka M, Murase T, Yoshida M, Sakairi M, Yamashita S, Yasuda Y, Yoshikawa A, Hayashi Y and Kakigami T <3 more 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 (- 3)
Ref: Bioorganic & Medicinal Chemistry, 19:7221, 2011 : PubMed
Abstract


ESTHER: Kato_2011_Bioorg.Med.Chem_19_7221
PubMedSearch: Kato 2011 Bioorg.Med.Chem 19 7221
PubMedID: 22019046
Inhibitor(s) related to this paper: Anagliptin

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.