Antihyperglycemic and Antihyperlipidemic Effects of Newly Synthesized Glibenclamide Analogues on Streptozotocin-diabetic Rats

A. Ahmadi; M. Khalili; M. Farsadrooh; M. Ghiasi; B. Nahri-Niknafs

doi:10.1055/s-0033-1349128

Drug Research, Table of Contents

Drug Res (Stuttg) 2013; 63(12): 614-619
DOI: 10.1055/s-0033-1349128

Original Article

Antihyperglycemic and Antihyperlipidemic Effects of Newly Synthesized Glibenclamide Analogues on Streptozotocin-diabetic Rats

A. Ahmadi

¹Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran

,

M. Khalili

²Department of Physiology, Neuroscience and Herbal Medicine Research Center, Shahed University, Tehran, Iran

,

M. Farsadrooh

¹Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran

,

M. Ghiasi

¹Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran

,

B. Nahri-Niknafs

¹Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran

› Author Affiliations

Abstract

In this study, new glibenclamide analogues (5a–d) with substituted pharmacological triethoxysilyl propan, allyl and ethoxyphenyl groups for cyclohexyl moiety have been synthesized by condensing sulfonamide (4) with related isocyanate or isothiocyanate’s compounds. The newly synthesized drugs were evaluated for their antihyperglycemic and antihyperlipidemic activities with streptozotocin (STZ)-induced diabetic rats. All showed hypoglycemic and hypolipidemic activities compared to the control animals but 5c and 5d exhibited more and significant lowering blood activities similar to glibenclamide. This was concerned with identical affinities to bind with SUR1 receptor. Moreover, the new drugs displayed high efficiency for reducing serum LDL level which resulted in a high HDL/LDL ratio as a good lipid profile compared to other groups.

Key words

glibenclamide - sulfonylurea - antihyperglycemic - antihyperlipidemic activities

Full Text

References

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