DOCKING STUDIES ON IMIDAZOLIDINE ANALOGUES FOR MANAGEMENT OF DIABETES

Apply

DOCKING STUDIES ON IMIDAZOLIDINE ANALOGUES FOR MANAGEMENT OF DIABETES

Journal Title: Journal of Drug Delivery and Therapeutics - Year 2017, Vol 7, Issue 7

Abstract

Glycogen synthase kinase-3β (GSK-3β) has recently emerged, in the field of medicinal chemistry, as one of the most attractive therapeutic targets for type II diabetes. Phenylmethylene hydantoins (PMHs) forms strong interactions with the hinge region of GSK-3β; carbonyl oxygen at position 2 form a H-bonding with backbone nitrogen of Val135 and the NH at position 3 to the carbonyl oxygen of Asp133. The hydantoin ring was sandwiched between Ala83, on top, and Leu188, on the bottom. The aromatic ring is rotated out of plane from the hydantoin plane, allowing extensive interactions with the nucleotide-binding loop. Furthermore, the substituted benzylidene ring system builds an H-bonding interaction with the guanidine moiety of Arg141. Targeting Arg141 is important to improve the activity in the process of designing new derivatives because it is considered the selectivity residue for GSK-3β.

Authors and Affiliations

Sumeet Prachand

Keywords

Croton sparsiflorus whole plant extract mediated biosynthesis of metallic silver nanoparticles and their antibacterial activity

In the present study, the potential of aqueous whole plant extract of Croton sparsiflorus for biosynthesis of silver nanoparticles (AgNPs) was evaluated. The formation of AgNPs was confirmed by color changes and UV- Visi...

EVALUATION OF CRYSTALLINE PENICILLIN UTILIZATION IN PEDIATRICS WARD OF TERTIARY CARE HOSPITAL OF EASTERN ETHIOPIA: THE CASE OF HIWOT FANA SPECIALIZED UNIVERSITY HOSPITAL

Background: Crystalline penicillin is one the commonly prescribed antibiotics that has been used for the treatment of certain susceptible bacterial infections over several years in Ethiopia. However, little is known abou...

EP ID EP300614
DOI -
Views 76
Downloads 0