edoc

Synthesis of a series of N(6)-substituted adenosines with activity against trypanosomatid parasites

Link, A. and Heidler, P. and Kaiser, M. and Brun, R.. (2009) Synthesis of a series of N(6)-substituted adenosines with activity against trypanosomatid parasites. European Journal of Medicinal Chemistry, 44 (9). pp. 3665-3671.

Full text not available from this repository.

Official URL: http://edoc.unibas.ch/dok/A5843344

Downloads: Statistics Overview

Abstract

The involvement of purine salvage in the accumulation of current trypanocidal drugs is important for the treatment of African sleeping sickness. The substrate specificity of essential nucleoside transporters is therefore of physiological and pharmacological interest. With the intention to contribute to the knowledge in the field, a series of 16 adenosine derivatives with substituents in N(6)-position were prepared in order to evaluate their potential to inhibit Trypanosoma brucei spp. in vitro. An unmodified ribose moiety was selected to conserve key molecular recognition motifs of the arsenal of integral membrane proteins expressed in large numbers on the protozoan plasma membrane. Two of the new compounds prepared using a polymer-assisted acylation protocol showed antitrypanosomal activities in the single digit micromolar concentration range
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Kaiser, Marcel
Item Type:Article, refereed
Bibsysno:Link to catalogue
Publisher:Elsevier
ISSN:0223-5234
Note:Publication type according to Uni Basel Research Database: Journal article
Related URLs:
Identification Number:
Last Modified:18 Oct 2017 07:14
Deposited On:14 Sep 2012 06:41

Repository Staff Only: item control page