Design, synthesis and antidiabetic evaluation of oxazolone derivatives

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.

(4Z)-4-Benzylidene-2-phenyl-1,3-oxazol-5(4H)-one

“…For background to the biological activity of oxazolone derivatives, see: Fidanza & Dernoeden (1996); Khan et al (2006); Puig et al (2000) For the synthesis, see: Mariappan et al (2011). Table 1 Hydrogen-bond geometry (Å , ).…”

Synthesis and Antioxidant Properties of New Oxazole-5(4<i>H</i>)-one Derivatives

“…All chemicals and solvents were purchased from commercial sources and used without furter purification. p-Fluorohippuric acid 11 , p-methylhippuric acid 12 , p-nitrohippuric acid 11 , p-chlorohippuric acid 13 , p-methoxyhippuric acid 14 and p-phenylhippuric acid 15 were prepared according to the literature. was dissolved in a 100 mL of 10% sodium hydroxide solution and appropriate benzoyl chloride (0.12 mol) was added portion-wise into it and the reaction mixture was shaked vigorously after each addition until all the chloride has been reacted for 1 h at 5°C and then at room temperature for 1 h, again.…”

“…[11][12][13][14][15] The synthetic route for hippuric acid derivatives (7-13) is displayed in Scheme 1.…”

Synthesis, Antioxidant and Antidiabetic Activity of 1-[(5-Substituted phenyl)-4,5-dihydro-1H-pyrazol-3-yl]-5-phenyl-1H-tetrazole

“…All the synthesized compounds were screened for in vivo antidiabetic activity by streptozotocin induced model in albino rat [38][39][40][41] .…”