title: Novel design principle validated: glucopyranosylidene-spiro-oxathiazole as new nanomolar inhibitor of glycogen phosphorylase, potential antidiabetic agent.
abstract: 2-Naphthyl-substituted glucopyranosylidene-spiro-oxathiazole prepared following a novel design principle was found to be the best known glucose analogue inhibitor of rabbit muscle glycogen phosphorylase b (K(i) 160 nM).
authors.affiliation: Department of Organic Chemistry, University of Debrecen, PO Box 20, H-4010 Debrecen, Hungary. somsak@tigris.unideb.hu
authors.forename: László
authors.initials: L
authors.lastname: Somsák
authors.forename: Veronika
authors.initials: V
authors.lastname: Nagy
authors.forename: Sébastien
authors.initials: S
authors.lastname: Vidal
authors.forename: Katalin
authors.initials: K
authors.lastname: Czifrák
authors.forename: Eszter
authors.initials: E
authors.lastname: Berzsényi
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Praly
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005947:Glucose / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006003:Glycogen / Q000737:chemistry; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007700:Kinetics; D008956:Models, Chemical; D011817:Rabbits; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D007004:Hypoglycemic Agents; D013141:Spiro Compounds; D013844:Thiazoles; C540068:glucopyranosylidene-spiro-oxathiazole; D006003:Glycogen; D024981:Glycogen Phosphorylase; D005947:Glucose