摘要

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 11 beta-HSD1. Pyrazole containing compounds can also act as competitive antagonist at cannabinoid-1 receptor while agonist at peroxisome proliferator-activated receptor-alpha and gamma. 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.

  • 出版日期2014-6