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Prodruggability of Carbohydrates - Oral FimH Antagonists
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 3707410
Author(s) Schönemann, Wojciech; Kleeb, Simon; Dätwyler, Philipp; Schwardt, Oliver; Ernst, Beat
Author(s) at UniBasel Ernst, Beat
Schwardt, Oliver
Schönemann, Wojciech
Kleeb, Simon
Dätwyler, Philipp
Year 2016
Title Prodruggability of Carbohydrates - Oral FimH Antagonists
Journal Canadian Journal of Chemistry
Volume 94
Number 11
Pages / Article-Number 909-919
Abstract The bacterial lectin FimH is a promising therapeutic target for the nonantibiotic prevention and treatment of urinary tract infections. In this communication, an ester prodrug approach is described to achieve oral bioavailability for FimH antagonists. By introducing short-chain acyl promoieties at the C-6 position of a biphenyl α- d -mannopyranoside, prodrugs with an excellent absorption potential were obtained. The human carboxylesterase 2 was identified as a main enzyme mediating rapid bioconversion to the active principle. Despite their propensity to hydrolysis within the enterocytes during absorption, these ester prodrugs present a considerable progress in the development of orally available FimH antagonists.
Publisher National Research Council
ISSN/ISBN 0008-4042 ; 1480-3291
edoc-URL http://edoc.unibas.ch/52929/
Full Text on edoc No
Digital Object Identifier DOI 10.1139/cjc-2015-0582
ISI-Number WOS:000388095300005
Document type (ISI) Article
 
   

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