Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities.
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.
Kumar
Atul
A
Medicinal and Process Chemistry Division, Central Drug Research Institute, P.O. Box 172, Lucknow 226001, Uttar Pradesh, India. dratulsax@gmail.com
Ahmad
Pervez
P
Maurya
Ram Awatar
RA
Singh
A B
AB
Srivastava
Arvind K
AK
D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D004791:Enzyme Inhibitors; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology; D008055:Lipids / Q000097:blood; D051379:Mice; D010080:Oxazoles / Q000737:chemistry* / Q000494:pharmacology; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D051381:Rats; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000097:blood
D004791:Enzyme Inhibitors; D007004:Hypoglycemic Agents; D008055:Lipids; D010080:Oxazoles; D014280:Triglycerides; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; C516609:Ptpn1 protein, mouse