Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities

Atul Kumar; Pervez Ahmad; Ram Awatar Maurya; A B Singh; Arvind K Srivastava

doi:10.1016/j.ejmech.2008.03.009

Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities

Eur J Med Chem. 2009 Jan;44(1):109-16. doi: 10.1016/j.ejmech.2008.03.009. Epub 2008 Mar 27.

Authors

Atul Kumar¹, Pervez Ahmad, Ram Awatar Maurya, A B Singh, Arvind K Srivastava

Affiliation

¹ Medicinal and Process Chemistry Division, Central Drug Research Institute, P.O. Box 172, Lucknow 226001, Uttar Pradesh, India. [email protected]

PMID: 18436346
DOI: 10.1016/j.ejmech.2008.03.009

Abstract

A series of 2-aryl-naphtho[1,2-d]oxazole derivatives have been synthesized and evaluated for PTP-1B inhibitory activity. The compounds have been screened in vivo for antidiabetic activity under sucrose loaded model (SLM), sucrose-challenged streptozotocin-induced diabetic rat model (STZ-S) and db/db mice model. Compounds 8 and 12 have shown promising PTP-1B inhibitory activity, significant antidiabetic activity, moderate lipid and triglyceride lowering activity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Diabetes Mellitus, Experimental / drug therapy*
Enzyme Inhibitors
Hypoglycemic Agents / chemistry*
Hypoglycemic Agents / pharmacology
Lipids / blood
Mice
Oxazoles / chemistry*
Oxazoles / pharmacology
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
Rats
Structure-Activity Relationship
Triglycerides / blood

Substances

Enzyme Inhibitors
Hypoglycemic Agents
Lipids
Oxazoles
Triglycerides
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Ptpn1 protein, mouse