The number compounds have been prepared in order to improve the pharmacological proﬁles of antihyperglycemic activity. The series of 3-benzyl-2-(4'-substituted phenyl)-4(5H)-(4''-nitrophenyl amino)-1, 3-oxazolidines 6a-e were tested against hyperglycemic activity. Their antihyperglycemic activity was evaluated by Streptozotocin (STZ) and Sucrose-loaded (SLM) model. The results of studies indicate that the compounds 6a, b, c, d, e displayed signiﬁcant reduction in blood glucose level in streptozotocin and sucrose loaded rat models. The purity of the synthesized compounds was characterized by means of IR, 1H-NMR, mass spectral and elemental analysis.