(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Data up to Jan 2025
Total Citations Per Year
Abstract
References (39)
Crystallography & NMR System: A New Software Suite for Macromolecular Structure Determination
1998 • 15,791 citations
MOLREP: an Automated Program for Molecular Replacement
1997 • 4,644 citations
Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and β-cell function in type 2 diabetes: a parallel-group study
2002 • 1,295 citations
Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV.
1995 • 1,064 citations
Both subcutaneously and intravenously administered glucagon-like peptide I are rapidly degraded from the NH2-terminus in type II diabetic patients and in healthy subjects
1995 • 705 citations
Truncated GLP-1 (proglucagon 78?107-amide) inhibits gastric and pancreatic functions in man
1993 • 661 citations
1-[[(3-Hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: A Potent, Selective, and Orally Bioavailable Dipeptidyl Peptidase IV Inhibitor with Antihyperglycemic Properties
2003 • 594 citations
Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26
2000 • 540 citations
Molecular cloning of fibroblast activation protein alpha, a member of the serine protease family selectively expressed in stromal fibroblasts of epithelial cancers.
1994 • 522 citations
The asymmetric synthesis of .alpha.-amino acids. Electrophilic azidation of chiral imide enolates, a practical approach to the synthesis of (R)- and (S)-.alpha.-azido carboxylic acids
1990 • 448 citations
Crystal structure of human dipeptidyl peptidase IV/CD26 in complex with a substrate analog
2002 • 396 citations
The effect of physiological levels of glucagon-like peptide-1 on appetite, gastric emptying, energy and substrate metabolism in obesity
2001 • 371 citations
Dipeptidyl Peptidase IV Inhibitor Treatment Stimulates β-Cell Survival and Islet Neogenesis in Streptozotocin-Induced Diabetic Rats
2003 • 337 citations
The crystal structure of dipeptidyl peptidase IV (CD26) reveals its functional regulation and enzymatic mechanism
2003 • 291 citations
Cloning, expression and chromosomal localization of a novel human dipeptidyl peptidase (DPP) IV homolog, DPP8
2000 • 269 citations
Enantioselective Syntheses of (R)‐Amino Acids Using <scp>L</scp>‐Valine as Chiral Agent
1981 • 249 citations
Structural Basis of Proline-Specific Exopeptidase Activity as Observed in Human Dipeptidyl Peptidase-IV
2003 • 223 citations
Genistein potentiates wild-type and delta F508-CFTR channel activity
1997 • 205 citations
Long-term inhibition of dipeptidyl peptidase IV improves glucose tolerance and preserves islet function in mice
2002 • 204 citations
Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII
2003 • 178 citations
Identification and characterization of human DPP9 , a novel homologue of dipeptidyl peptidase IV
2002 • 135 citations
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: A Potent, Selective, and Orally Bioavailable Dipeptidyl Peptidase IV Inhibitor with Antihyperglycemic Properties
2002 • 119 citations
Purification of Dipeptidyl Aminopeptidase II (Dipeptidyl Arylamidase II) of the Anterior Pituitary Gland
1968 • 111 citations
Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability: Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α-Aminoacyl-<scp>l</scp>-cis-4,5-methanoprolinenitrile-Based Inhibitors
2004 • 100 citations
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors
2004 • 93 citations
Aminomethylpyrimidines as novel DPP-IV inhibitors: A 105-fold activity increase by optimization of aromatic substituents
2004 • 79 citations
Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors
2004 • 74 citations
Inhibition of dipeptidyl peptidase IV (DPP IV) by 2-(2-amino-1-fluoro-propylidene)-cyclopentanecarbonitrile, a fluoroolefin containing peptidomimetic
2003 • 64 citations
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors
2004 • 57 citations
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors
2003 • 42 citations
1,2,4-Triazoles. VI.1 The Synthesis of Some s-Triazolo[4,3-a]pyrazines
1962 • 35 citations
An aminomethylpyrimidine DPP-IV inhibitor with improved properties
2004 • 35 citations
Synthesis of 1,6‐Disubstituted Cycloheptatriene Derivatives from Benzocyclopropene
1981 • 28 citations
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors
2004 • 28 citations
Synthesis and evaluation of the thiosemicarbazone, dithiocarbazonate, and 2'-pyrazinylhydrazone of pyrazinecarboxaldehyde as agents for the treatment of iron overload
1979 • 27 citations
Synthesis of C-nucleosides. 17. s-Triazolo[4,3-a]pyrazines
1979 • 27 citations
4-cyanothiazolidides as very potent, stable inhibitors of dipeptidyl peptidase IV
1996 • 24 citations
1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors
2000 • 14 citations
ChemInform Abstract: Synthesis of Fmoc‐β‐Homoamino Acids by Ultrasound‐Promoted Wolff Rearrangement.
1998 • 7 citations