title: Antihyperglycemic and antihyperlipidemic effects of newly synthesized glibenclamide analogues on streptozotocin-diabetic rats.
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.
authors.affiliation: Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran.
authors.forename: A
authors.initials: A
authors.lastname: Ahmadi
authors.affiliation: Department of Physiology, Neuroscience and Herbal Medicine Research Center, Shahed University, Tehran, Iran.
authors.forename: M
authors.initials: M
authors.lastname: Khalili
authors.affiliation: Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran.
authors.forename: M
authors.initials: M
authors.lastname: Farsadrooh
authors.affiliation: Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran.
authors.forename: M
authors.initials: M
authors.lastname: Ghiasi
authors.affiliation: Department of Chemistry, Faculty of Science, Islamic Azad University, Karaj Branch, Karaj, Iran.
authors.forename: B
authors.initials: B
authors.lastname: Nahri-Niknafs
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D008076:Cholesterol, HDL / Q000097:blood; D008078:Cholesterol, LDL / Q000097:blood / Q000187:drug effects; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy* / Q000503:physiopathology; D005905:Glyburide / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051381:Rats; D013311:Streptozocin; D013329:Structure-Activity Relationship; D064233:Sulfonylurea Receptors / Q000378:metabolism
chemical_list: C577509:Abcc8 protein, rat; D001786:Blood Glucose; D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D064233:Sulfonylurea Receptors; D013311:Streptozocin; D005905:Glyburide