"It is now clear that aggressive control of hyperglycemia in patients with diabetes can prevent or delay the onset of complications such as retinopathy, nephropathy, and neuropathy (Kumar et al., 2007). We have found that oxazolidines and related oxazolidine are classes of heterocycles that are of considerable interest because of the diverse range of their biological properties, such as antihypertensive (Caroon et al., 1983), antidepressant (Pinder, 1985), antithyroid (Gardrat and Latxague, 1990), leishmanicidal (Sonika and Satyavan, 1990), antidiabetic (Heong et al., 2007), anti-HIV (Sharma et al., 2003), antiarrhythmic (Kostochka et al., 2003), antitumor (Vara Prasad et al., 2006), and anticonvulsant and antimicrobial (Kim et al., 2008). "
[Show abstract][Hide abstract] ABSTRACT: A number of compounds have been prepared in order to improve pharmacological roles of antihyperglycemic activity. In the present paper, a series of 3-benzyl-2-(4'-substituted phenyl)-4(5H)-(4″-nitrophenyl amino)-1,3-oxazolidines (6a-e) were tested against hyperglycemia. Their antihyperglycemic activity was evaluated by streptozotocin (STZ) and sucrose-loaded (SLM) models. Compounds 6a, b, c, d, and e displayed significant reductions in blood glucose in the streptozotocin and sucrose loaded rat models. The purity of the synthesized compounds was characterized by means of IR, (1)H-NMR, mass spectral and elemental analysis.
Archives of Pharmacal Research 06/2011; 34(6):887-91. DOI:10.1007/s12272-011-0604-3 · 1.75 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: A novel series of conformationally restricted oxazolidinones was synthesized, in which the heterocyclic D ring was substituted with various amino groups. Several analogs exhibited potent activity against both gram-positive and fastidious gram-negative organisms. Certain amino-substituted analogs also exhibited improved aqueous solubility compared to the corresponding un-substituted heterocyclic D-ring analogs.
[Show abstract][Hide abstract] ABSTRACT: A novel series of conformationally-restricted oxazolidinones was synthesized which possess a fused pyrazole ring substituted with various alkyl, aryl and heteroaryl substituents. A number of analogs exhibited potent activity against both gram-positive and fastidious gram-negative organisms.
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