pyrimidinones and alogliptin

pyrimidinones has been researched along with alogliptin* in 1 studies

Other Studies

1 other study(ies) available for pyrimidinones and alogliptin

Article	Year
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. Journal of medicinal chemistry, 2007, May-17, Volume: 50, Issue:10 Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4). Herein, we describe the structure-based design and optimization of alogliptin and related quinazolinone-based DPP-4 inhibitors. Following an oral dose, these noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and a lowering of blood glucose in animal models of diabetes. Alogliptin is currently undergoing phase III trials in patients with type 2 diabetes. Topics: Animals; Binding Sites; Blood Glucose; Cytochrome P-450 Enzyme Inhibitors; Diabetes Mellitus, Experimental; Dipeptidyl Peptidase 4; Dipeptidyl-Peptidase IV Inhibitors; Dogs; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Female; Glucose Tolerance Test; Haplorhini; Humans; Hypoglycemic Agents; In Vitro Techniques; Mice; Microsomes, Liver; Models, Molecular; Piperidines; Pyrimidinones; Quinazolinones; Rats; Rats, Wistar; Structure-Activity Relationship; Uracil	2007

Article

Year

Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.

Journal of medicinal chemistry, 2007, May-17, Volume: 50, Issue:10

Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4). Herein, we describe the structure-based design and optimization of alogliptin and related quinazolinone-based DPP-4 inhibitors. Following an oral dose, these noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and a lowering of blood glucose in animal models of diabetes. Alogliptin is currently undergoing phase III trials in patients with type 2 diabetes.

Topics: Animals; Binding Sites; Blood Glucose; Cytochrome P-450 Enzyme Inhibitors; Diabetes Mellitus, Experimental; Dipeptidyl Peptidase 4; Dipeptidyl-Peptidase IV Inhibitors; Dogs; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Female; Glucose Tolerance Test; Haplorhini; Humans; Hypoglycemic Agents; In Vitro Techniques; Mice; Microsomes, Liver; Models, Molecular; Piperidines; Pyrimidinones; Quinazolinones; Rats; Rats, Wistar; Structure-Activity Relationship; Uracil

2007