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.
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