Synthesis of a new transition-state analog of the sialyl donor. Inhibition of sialyltransferases

Autor:	Katie E. Amaral, Benjamin A. Horenstein, Hongbin Sun, Jingsong Yang
Rok vydání:	2001
Předmět:	Transition (genetics) biology Chemistry Stereochemistry Organic Chemistry Glycosyltransferase inhibitor Biochemistry Combinatorial chemistry Transition state Transition state analog Drug Discovery Glycosyltransferase biology.protein Carbonylation
Zdroj:	Tetrahedron Letters. 42:2451-2453
ISSN:	0040-4039
Popis:	A new class of glycosyltransferase inhibitor has been designed and synthesized. The designed inhibitors 3a / 3b provide conformational mimicry of the transition state in sialyltransfer reactions. The key synthetic steps involve a Meinwald rearrangement and a palladium-catalyzed carbonylation reaction. The results of kinetic studies show that 3a / 3b exhibit significant inhibition on both 2,3- and 2,6-sialytransferases.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::46fad08a0f45140f913593ffa494ca90 https://doi.org/10.1016/s0040-4039(01)00204-0 Zobrazit plný text záznamu Full Text from ScienceDirect