dc.contributor.author | Papadopoulou, MV | en_US |
dc.contributor.author | Bloomer, WD | en_US |
dc.contributor.author | Rosenzweig, HS | en_US |
dc.contributor.author | WILKINSON, SR | en_US |
dc.contributor.author | Szular, J | en_US |
dc.contributor.author | Kaiser, M | en_US |
dc.date.accessioned | 2016-04-14T08:28:38Z | |
dc.date.available | 2016-04-05 | en_US |
dc.date.issued | 2016-07-19 | en_US |
dc.date.submitted | 2016-04-07T15:05:22.552Z | |
dc.identifier.issn | 0223-5234 | en_US |
dc.identifier.uri | http://qmro.qmul.ac.uk/xmlui/handle/123456789/11848 | |
dc.description.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 anti-trypanosomatid agents. All tested compounds were active or moderately active against Trypanosoma cruzi amastigotes in infected L6 cells and Trypanosoma brucei brucei, four were moderately active against Leishmania donovani axenic parasites while none were deemed active against Trypanosoma brucei rhodesiense. For the most active/moderately active compounds a moderate selectivity against the human infectious parasites was observed. There was a good correlation between lipophilicity (clogP value) versus antileishmanial activity and mammalian cell toxicity with a similar correlation also noted 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. | en_US |
dc.description.sponsorship | This work was supported in part by internal funds of the Radiation Medicine Department at NorthShore University HealthSystem. In addition, the Drugs for Neglected Diseases initiative (DNDi) received financial support from the Bill and Melinda Gates Foundation to perform the in vitro screenings against parasites. | en |
dc.format.extent | 179 - 186 (8) | en_US |
dc.language.iso | en | en |
dc.publisher | Elsevier | en_US |
dc.relation.ispartof | European Journal of Medicinal Chemistry | en_US |
dc.rights | © 2016. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ | |
dc.title | Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds | en_US |
dc.type | Article | |
dc.rights.holder | Copyright © 2016 Published by Elsevier Masson SAS | |
dc.identifier.doi | 10.1016/j.ejmech.2016.04.010 | en_US |
pubs.notes | Not known | en_US |
pubs.publication-status | Published | en_US |
pubs.publisher-url | http://dx.doi.org/10.1016/j.ejmech.2016.04.010 | en_US |
pubs.volume | 117 | en_US |
dcterms.dateAccepted | 2016-04-05 | en_US |