title: Design, Synthesis and in Vivo Evaluation of Novel Glycosylated Sulfonylureas as Antihyperglycemic Agents.
abstract: Sulphonylurea compounds have versatile activities such as antidiabetic, diuretic, herbicide, oncolytic, antimalarial, antifungal and anticancer. The present study describes the design, synthesis and in vivo testing of novel glycosylated aryl sulfonylurea compounds as antihyperglycaemic agents in streptozocine-induced diabetic mice. The rational for the introduction of the glucosamine moiety is to enhance selective drug uptake by pancreatic β-cells in order to decrease the cardiotoxic side effect commonly associated with sulfonylurea agents. 2-Deoxy-2-(4-chlorophenylsulfonylurea)-D-glucopyranose was found to be the most potent antihyperglycaemic agents among the synthesized compounds in diabetic mice. This investigation indicates the importance of this novel class as potential antihyperglycaemic agents.
authors.affiliation: Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman 11942, Jordan. gh.suaifan@ju.edu.jo.
authors.forename: Ghadeer A R Y
authors.initials: GA
authors.lastname: Suaifan
authors.affiliation: Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman 11942, Jordan. m.shehadeh@ju.edu.jo.
authors.forename: Mayadah B
authors.initials: MB
authors.lastname: Shehadeh
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, The University of Jordan, Amman 11942, Jordan. rulamdarwish@yahoo.com.
authors.forename: Rula M
authors.initials: RM
authors.lastname: Darwish
authors.affiliation: Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman 11942, Jordan.
authors.forename: Hebah
authors.initials: H
authors.lastname: Al-Ijel
authors.affiliation: Institute of Pharmaceutical Science, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK. vincenzo.abbate@kcl.ac.uk.
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Abbate
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D003921:Diabetes Mellitus, Experimental; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy / Q000378:metabolism; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006031:Glycosylation; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D013453:Sulfonylurea Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D013453:Sulfonylurea Compounds
keywords: antihyperglycemic agents; glucosamine; streptozocine; sulphonylurea