Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 3501323
Author(s) Papadopoulou, Maria V.; Bloomer, William D.; Rosenzweig, Howard S.; Wilkinson, Shane R.; Szular, Joanna; Kaiser, Marcel
Author(s) at UniBasel Kaiser, Marcel
Year 2016
Title Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds
Journal European journal of medicinal chemistry
Volume 117
Pages / Article-Number 179-86
Abstract A small series of 5-nitro-2-aminothiazole-based amides containing arylpiperazine-, biphenyl- or aryloxyphenyl groups in their core were synthesized and evaluated as antitrypanosomatid agents. All tested compounds were active or moderately active against Trypanosoma cruzi amastigotes in infected L6 cells and Trypanosoma brucei brucei, four of eleven compounds were moderately active against Leishmania donovani axenic parasites while none were deemed active against T. brucei rhodesiense. For the most active/moderately active compounds a moderate selectivity against each parasite was observed. There was good correlation between lipophilicity (clogP value) and antileishmanial activity or toxicity against L6 cells. Similarly, good correlation existed between clogP values and IC50 values against T. cruzi in structurally related subgroups of compounds. Three compounds were more potent as antichagasic agents than benznidazole but were not activated by the type I nitrorectusase (NTR).
Publisher Elsevier
ISSN/ISBN 0223-5234
edoc-URL http://edoc.unibas.ch/42520/
Full Text on edoc No
Digital Object Identifier DOI 10.1016/j.ejmech.2016.04.010
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/27092415
ISI-Number WOS:000376837800015
Document type (ISI) Journal Article
 
   

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