sitagliptin-phosphate and 2-amino-4-phenylbutyric-acid

sitagliptin-phosphate has been researched along with 2-amino-4-phenylbutyric-acid* in 1 studies

Other Studies

1 other study(ies) available for sitagliptin-phosphate and 2-amino-4-phenylbutyric-acid

Article	Year
Design, synthesis, and pharmacological evaluation of highly potent and selective dipeptidyl peptidase-4 inhibitors. Archiv der Pharmazie, 2015, Volume: 348, Issue:6 The optimization of a series of fused β-homophenylalanine inhibitors of dipeptidyl peptidase-4 (DPP-4) is described. Modification on the P2-binding moiety of 6 (IC50 = 10 nM) led to the discovery of β-homophenylalanine derivatives containing pyrrolidin-2-ylmethyl amides. The introduction of a sulfamine in the meta position of the phenyl ring improved the potency against DPP-4 (6-12-fold increase). Compound 14k showed DPP-4 inhibitory activity with an IC50 value of 0.87 nM. Meanwhile, in vivo experiments exhibited that 14h had an efficiency comparable to sitagliptin at the dose of 10 mg/kg. Topics: Aminobutyrates; Animals; Binding Sites; Biomarkers; Blood Glucose; Caco-2 Cells; Dipeptidyl Peptidase 4; Dipeptidyl-Peptidase IV Inhibitors; Drug Design; Humans; Male; Mice, Inbred C57BL; Molecular Docking Simulation; Protein Binding; Protein Conformation; Sitagliptin Phosphate; Structure-Activity Relationship; Time Factors	2015

Article

Year

Design, synthesis, and pharmacological evaluation of highly potent and selective dipeptidyl peptidase-4 inhibitors.

Archiv der Pharmazie, 2015, Volume: 348, Issue:6

The optimization of a series of fused β-homophenylalanine inhibitors of dipeptidyl peptidase-4 (DPP-4) is described. Modification on the P2-binding moiety of 6 (IC50 = 10 nM) led to the discovery of β-homophenylalanine derivatives containing pyrrolidin-2-ylmethyl amides. The introduction of a sulfamine in the meta position of the phenyl ring improved the potency against DPP-4 (6-12-fold increase). Compound 14k showed DPP-4 inhibitory activity with an IC50 value of 0.87 nM. Meanwhile, in vivo experiments exhibited that 14h had an efficiency comparable to sitagliptin at the dose of 10 mg/kg.

Topics: Aminobutyrates; Animals; Binding Sites; Biomarkers; Blood Glucose; Caco-2 Cells; Dipeptidyl Peptidase 4; Dipeptidyl-Peptidase IV Inhibitors; Drug Design; Humans; Male; Mice, Inbred C57BL; Molecular Docking Simulation; Protein Binding; Protein Conformation; Sitagliptin Phosphate; Structure-Activity Relationship; Time Factors

2015