Design, synthesis and antidiabetic evaluation of oxazolone derivatives

G MARIAPPAN^a*, B P SAHA^a, SRIPARNA DATTA^a, DEEPAK KUMAR^a and P K HALDAR^b

^aDepartment of Medicinal Chemistry, ^bDepartment of Pharmacology, Himalayan Pharmacy Institute, East Sikkim 737 136, India

*Corresponding author. E-mail: gmariappanhpi@yahoo.co.in

MS received 1 December 2010; revised 16 March 2011; accepted 18 March 2011

Abstract. A series of ten novel (2a–j) 4-arylidine 2-[4-methoxy phenyl] oxazol-5-one derivatives were synthesized and assayed in vivo to investigate their antidiabetic activities by streptozotocin-induced model in rat. These derivatives showed considerable biological efficacy when compared to rosiglitazone, a potent and wellknown antidiabetic agent as a reference drug. All the compounds were effective, amongst them 2d shows more prominent activity at 50 mg/k.g.p.o. The experimental results are statistically significant at P < 0.01 level.

Graphical Abstract. A series of oxazolones derivatives have been synthesized and evaluated for antidiabetic activity.

Keywords. Oxazolone scaffold; acetyl glycine; hypoglycemic activity; antiinflammatory.