DOCKING STUDIES ON IMIDAZOLIDINE ANALOGUES FOR MANAGEMENT OF DIABETES

  • Sumeet Prachand Suresh Gyan Vihar University, Jaipur, India
  • Ritu Gilhotra Suresh Gyan Vihar University, Jaipur, India
  • Arun Gupta School of Pharmacy, Dr. APJ Abdul Kalam University, Indore, India
  • Sanjay Jain Indore Institute of Pharmacy, Indore, India

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.

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Author Biographies

Sumeet Prachand, Suresh Gyan Vihar University, Jaipur, India
Suresh Gyan Vihar University, Jaipur, India
Ritu Gilhotra, Suresh Gyan Vihar University, Jaipur, India
Suresh Gyan Vihar University, Jaipur, India
Arun Gupta, School of Pharmacy, Dr. APJ Abdul Kalam University, Indore, India

School of Pharmacy, Dr. APJ Abdul Kalam University, Indore, India

Sanjay Jain, Indore Institute of Pharmacy, Indore, India

Indore Institute of Pharmacy, Indore, India

References

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How to Cite
Prachand, S., Gilhotra, R., Gupta, A., & Jain, S. (2017). DOCKING STUDIES ON IMIDAZOLIDINE ANALOGUES FOR MANAGEMENT OF DIABETES. Journal of Drug Delivery and Therapeutics, 7(7), 128-130. https://doi.org/10.22270/jddt.v7i7.1610