Abstract
Pyrazole scaffold containing compounds have been found to be as enzyme activator or inhibitor in the diabetic disease condition. The pyrazole containing compounds have been found to be activators in case such as glucokinase and as inhibitors in cases such as sodium glucose co-transporter-1, sodium-glucose co-transporter-2, dipeptidyl peptidase-4, glycogen synthase kinase-3beta, Glucagon-stimulated intracellular cAMP formation and 11β-HSD1. Pyrazole containing compounds can also act as competitive antagonist at cannabinoid-1 receptor while agonist at peroxisome proliferatoractivated receptor-α and γ. In present work, the most active pyrazole derivatives have been selected from reported literature along with methods utilized for detection of blood plasma glucose levels or urinary glucose levels as well as assays involving enzyme inhibition or activation at cellular level. The activity values of corresponding pyrazole compounds obtained from synthetic or structural activity relationship studies can be helpful for medicinal chemist to focus design of novel chemical entities containing pyrazole system as a part of antidiabetic drug substance.
Keywords: Pyrazole, antidiabetic, Sodium glucose co- transporter, Peroxisome proliferator-activated receptor, Glycogen synthase kinase, Dipeptidyl peptidase-4.
Letters in Drug Design & Discovery
Title:Development of Pyrazole Compounds as Antidiabetic Agent: A Review
Volume: 11 Issue: 5
Author(s): Prasanna A. Datar and Sonali R. Jadhav
Affiliation:
Keywords: Pyrazole, antidiabetic, Sodium glucose co- transporter, Peroxisome proliferator-activated receptor, Glycogen synthase kinase, Dipeptidyl peptidase-4.
Abstract: Pyrazole scaffold containing compounds have been found to be as enzyme activator or inhibitor in the diabetic disease condition. The pyrazole containing compounds have been found to be activators in case such as glucokinase and as inhibitors in cases such as sodium glucose co-transporter-1, sodium-glucose co-transporter-2, dipeptidyl peptidase-4, glycogen synthase kinase-3beta, Glucagon-stimulated intracellular cAMP formation and 11β-HSD1. Pyrazole containing compounds can also act as competitive antagonist at cannabinoid-1 receptor while agonist at peroxisome proliferatoractivated receptor-α and γ. In present work, the most active pyrazole derivatives have been selected from reported literature along with methods utilized for detection of blood plasma glucose levels or urinary glucose levels as well as assays involving enzyme inhibition or activation at cellular level. The activity values of corresponding pyrazole compounds obtained from synthetic or structural activity relationship studies can be helpful for medicinal chemist to focus design of novel chemical entities containing pyrazole system as a part of antidiabetic drug substance.
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Cite this article as:
Datar A. Prasanna and Jadhav R. Sonali, Development of Pyrazole Compounds as Antidiabetic Agent: A Review, Letters in Drug Design & Discovery 2014; 11 (5) . https://dx.doi.org/10.2174/1570180810666131113212354
DOI https://dx.doi.org/10.2174/1570180810666131113212354 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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