Antiprotozoal selectivity of diimidazoline N-phenylbenzamides

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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
edoc-URL	http://edoc.unibas.ch/41608/
Full Text on edoc	No
Digital Object Identifier DOI	10.1021/id500034v
PubMed ID	http://www.ncbi.nlm.nih.gov/pubmed/27622464
ISI-Number	WOS:000368463300003
Document type (ISI)	Journal Article

20/04/2024

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