Current Issue : January-March Volume : 2018 Issue Number : 1 Articles : 3 Articles
In this survey, all types of cyclic compounds (aliphatic and aromatic) which containing one or more heteroatoms like (sulfur, nitrogen, oxygen, selenium), nomenclature of heterocyclic compounds as well as various membered rings. In recent advances there are various heterocyclic containing drugs used as biological as well as pharmacological activity like antifungal, anti-inflammatory, antibacterial, anticonvulsant, antiallergic, herbicidal, anticancer activity....
By 2030, the World Health Organization predicts more than 300 million people to be diagnosed with type 2 diabetes. The current therapeutic agents (like Insulin, Sulphonylureas, Biguanides, �±-Glucosidase inhibitors, PPAR agonist and GLP-1 agonist), although effective in increasing insulin secretion, are associated with some safety issue and undesirable side effects, including hypoglycemia, abnormalities in cardiovascular responses and �²-cell apoptosis. DPP-4 inhibitors offer several potential advantages over existing therapies including decreased risk of hypoglycemia, potential for weight loss and the potential for regeneration and differentiation of pancreatic �²-cells. Moreover, DPP-4 inhibitors can also be administered orally. Hence, Dipeptidyl peptidase-4 (DPP-4) inhibitors are new promising strategy for antidiabetic activity and several drugs are in the developmental stage. The present work involves the synthesis of 2-cyano pyrrolidine derivatives. Among all DPP-4 inhibitor derivatives, 2-Cyano pyrrolidine-based inhibitors have been studied most extensively. Apart from behaving as a proline mimic, the presence of the nitrile on the five-membered ring was shown to provide (i) nanomolar inhibition of DPP-4 and (ii) chemical stability adequate for oral administration. These intermediates fused with quinazolin-4-one derivative. The synthesized DPP-4 inhibitor derivative was evaluated by fluorescence assay using Gly-Pro-AMC as a DPP-4-specific fluorescent substrate....
The current therapeutic agents for type 2 diabetes (like Insulin, Sulphonylureas, Biguanides, �±-Glucosidase inhibitors, PPAR agonist and GLP-1 agonist), although effective in increasing insulin secretion, are associated with some safety issue and undesirable side effects, including hypoglycemia, abnormalities in cardiovascular responses and �²-cell apoptosis. DPP-4 inhibitors offer several potential advantages over existing therapies including decreased risk of hypoglycemia, potential for weight loss and the potential for regeneration and differentiation of pancreatic �²-cells. Moreover, DPP-4 inhibitors can also be administered orally. Among all DPP-4 inhibitor derivatives, 2-Cyano pyrrolidine-based inhibitors have been studied most extensively. Apart from behaving as a proline mimic, the presence of the nitrile on the five-membered ring was shown to provide (i) nanomolar inhibition of DPP-4 and (ii) chemical stability adequate for oral administration. These intermediate was fused with 2-amino-5-aryl-1, 3, 4-thiadiazole derivative to get series of novel 1-(2-(5-aryl-1,3,4-thiadiazol-2-ylamino)acetyl)pyrrolidine-2-carbonitrile derivatives. The synthesized DPP-4 inhibitor derivatives were evaluated by fluorescence assay using Gly-Pro-AMC as a DPP-4-specific fluorescent substrate....
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