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Prodruggability of Carbohydrates - Oral FimH Antagonists

Schönemann, Wojciech and Kleeb, Simon and Dätwyler, Philipp and Schwardt, Oliver and Ernst, Beat. (2016) Prodruggability of Carbohydrates - Oral FimH Antagonists. Canadian Journal of Chemistry, 94 (11). pp. 909-919.

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Official URL: http://edoc.unibas.ch/52929/

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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.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molekulare Pharmazie (Ernst)
UniBasel Contributors:Ernst, Beat and Schwardt, Oliver and Schönemann, Wojciech and Kleeb, Simon and Dätwyler, Philipp
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:National Research Council
ISSN:0008-4042
e-ISSN:1480-3291
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:28 Nov 2017 11:15
Deposited On:30 Oct 2017 07:30

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