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Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents

Papadopoulou, Maria V. and Bloomer, William D. and Lepesheva, Galina I. and Rosenzweig, Howard S. and Kaiser, Marcel and Aguilera-Venegas, Benjamín and Wilkinson, Shane R. and Chatelain, Eric and Ioset, Jean-Robert. (2015) Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents. Journal of medicinal chemistry, 58 (3). pp. 1307-1319.

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Official URL: http://edoc.unibas.ch/dok/A6357934

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Abstract

3-Nitro-1H-1,2,4-triazole-based amides with a linear, rigid core and 3-nitrotriazole-based fluconazole analogues were synthesized as dual functioning antitrypanosomal agents. Such compounds are excellent substrates for type I nitroreductase (NTR) located in the mitochondrion of trypanosomatids and, at the same time, act as inhibitors of the sterol 14α-demethylase (T. cruzi CYP51) enzyme. Because combination treatments against parasites are often superior to monotherapy, we believe that this emerging class of bifunctional compounds may introduce a new generation of antitrypanosomal drugs. In the present work, the synthesis and in vitro and in vivo evaluation of such compounds is discussed.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:05 Dec 2017 10:46
Deposited On:10 Apr 2015 09:13

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