vildagliptin and Diabetes-Mellitus

Diabetes is one of the major diseases worldwide and is the third leading cause of death in the United States. Anti-diabetic drugs are used in the treatment of diabetes mellitus to control glucose levels in the blood. Most of the drugs are administered orally, except for a few of them, such as insulin, exenatide, and pramlintide. In this review, we are going to discuss seven major types of anti-diabetic drugs: Peroxisome proliferator-activated receptor (PPAR) agonist, protein tyrosine phosphatase 1B (PTP1B) inhibitors, aldose reductase inhibitors, α-glucosidase inhibitors, dipeptidyl peptidase IV (DPP-4) inhibitors, G protein-coupled receptor (GPCR) agonists and sodium-glucose co-transporter (SGLT) inhibitors. Here, we are also discussing some of the recently reported anti-diabetic agents with its multi-target pharmacological actions. This review summarises recent approaches and advancement in anti-diabetes treatment concerning characteristics, structure-activity relationships, functional mechanisms, expression regulation, and applications in medicine.

Topics: Diabetes Mellitus; Dose-Response Relationship, Drug; Humans; Hypoglycemic Agents; Molecular Structure; Structure-Activity Relationship

The synthesis and biochemical evaluation of novel cyanothiazolidine inhibitors of dipeptidyl peptidase 4 (DPP4) is described. Their main structural feature is a constrained bicyclic core that prevents the intramolecular formation of inactive cyclic species. The inhibitors show good to moderate biochemical potency against DPP4 and display distinct selectivity profiles towards DPP7, DPP8 and DPP9 depending on their substitution.

Topics: Azabicyclo Compounds; Catalysis; Diabetes Mellitus; Dipeptidyl-Peptidase IV Inhibitors; Drug Design; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Models, Chemical; Molecular Structure; Nitriles; Protein Structure, Tertiary; Pyrrolidines; Structure-Activity Relationship; Thiazoles; Thiazolidines; Time Factors