Drug Res (Stuttg) 2013; 63(12): 614-619
DOI: 10.1055/s-0033-1349128
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

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

A. Ahmadi
1   Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran
,
M. Khalili
2   Department of Physiology, Neuroscience and Herbal Medicine Research Center, Shahed University, Tehran, Iran
,
M. Farsadrooh
1   Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran
,
M. Ghiasi
1   Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran
,
B. Nahri-Niknafs
1   Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran
› Author Affiliations
Further Information

Publication History

received 09 March 2013

accepted 14 June 2013

Publication Date:
04 July 2013 (online)

Preview

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.