Development of Voglibose (Basen), an Antidiabetic Agent

Autor:	Hiroshi Fukase
Rok vydání:	1997
Předmět:	Chemistry Valienamine Organic Chemistry Pharmacology medicine.disease Disaccharidase Sucrase chemistry.chemical_compound Postprandial Biochemistry Diabetes mellitus Voglibose medicine Stereoselectivity Maltase medicine.drug
Zdroj:	Journal of Synthetic Organic Chemistry, Japan. 55:920-925
ISSN:	1883-6526 0037-9980
Popis:	Voglibose (1, N- [2-hydroxy-1- (hydroxymethyl) ethyl] valiolamine, basen®), having more potent disaccharidase inhibitory activity against maltase and sucrase than do naturally occurring pseudo-oligosaccharide α-glucosidase inhibitors, has been developed for the treatment of diabetes mellitus as the blood glucose ameliorating agent. Valiolamine (2), an important key compound for the preparation of N-substituted valiolamine derivatives such as 1, was synthesized by stereoselective hydration of the carbon-carbon double bond of valienamine (3) obtained by microbiological degradation of validamycins. Efficient and practical total synthesis of 2 starting from D-glucose has also been achieved.In animals and healthy volunteers, voglibose (1) significantly reduced postprandial blood glucose concentration. Clinical trials in patients with diabetes mellitus also demonstrated that 1 improves post-pratial glucose levels. In Japan, 1 was approved in July, 1994.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::486bdd5ac36cd2b6ca60d60fcebc86aa https://doi.org/10.5059/yukigoseikyokaishi.55.920 Zobrazit plný text záznamu