Delving into the Latest Updates on Compound 14d(Beijing Institute Of Technology ) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

AKR1B1 x α-glucosidase

Action

inhibitors

Mechanism

AKR1B1 inhibitors(Aldose reductase inhibitors), α-glucosidase inhibitors(Acidic alpha-glucosidase inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Complications

Inactive Indication-

Originator Organization

Beijing Institute of Technology

Active Organization

Beijing Institute of Technology

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

We designed a novel series of bifunctional inhibitors of α-glucosidase and aldose reductase (ALR2) based on the structure of hydroxychalcone. The two enzymes relate to blood glucose level and anomalously elevated polyol pathway of glucose metabolism under hyperglycemia, respectively. Most compounds in the series exhibited a potent inhibitory activity for both enzymes, and a significant antioxidant property was shown. Further in vivo studies of 11j and 14d using streptozotocin (STZ)-induced diabetic rats as a model found that 11j achieved not only good antihyperglycemic and glucose tolerance effect in a dose-dependent manner (p < 0.01) but also showed effective inhibition of polyol pathway. 14d significantly suppressed the maltose-induced postprandial glucose elevation. Additionally, they effectively improved lipid metabolisms and restored an antioxidant ability. Therefore, the two compounds may be promising agents for the prevention and treatment of diabetic complications.

100 Deals associated with Compound 14d(Beijing Institute Of Technology )

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