Antiprotozoal selectivity of diimidazoline N-phenylbenzamides
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
ID 3396804
Author(s) Wang, Xiaofang; Dong, Yuxiang; Cal, Monica; Kaiser, Marcel; Wittlin, Sergio; Vennerstrom, Jonathan L
Author(s) at UniBasel Kaiser, Marcel
Wittlin, Sergio
Year 2015
Title Antiprotozoal selectivity of diimidazoline N-phenylbenzamides
Journal ACS infectious diseases
Volume 1
Number 3
Pages / Article-Number 135-9
Abstract We discovered three diimidazolines with high antiplasmodial selectivity that had IC50 values of 1.9-28 nM against cultured Plasmodium falciparum. We also identified a gem-dimethyl diimidazolines with high antitrypanosomal selectivity that had an IC50 value of 26 nM against cultured Trypanosoma brucei rhodesiense. Two 2-imidazoline heterocycles in a para orientation on a N-phenylbenzamide or similar core structure were required for high antiprotozoal activity. Ring expansion of the imidazoline as well as heterocyclic variants with pK(a) values of < 7 all decreased activity significantly.
Publisher ACS Publications
ISSN/ISBN 2373-8227
Full Text on edoc No
Digital Object Identifier DOI 10.1021/id500034v
PubMed ID
ISI-Number WOS:000368463300003
Document type (ISI) Journal Article

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