Synthesis and activity of 1H-benzimidazole and 1H-benzotriazole derivatives as inhibitors of Acanthamoeba castellanii

Katarzyna Kopańska; Andzelika Najda; Justyna Zebrowska; Lidia Chomicz; Janusz Piekarczyk; Przemysław Myjak; Maria Bretner

doi:10.1016/j.bmc.2004.03.022

Synthesis and activity of 1H-benzimidazole and 1H-benzotriazole derivatives as inhibitors of Acanthamoeba castellanii

Bioorg Med Chem. 2004 May 15;12(10):2617-24. doi: 10.1016/j.bmc.2004.03.022.

Authors

Katarzyna Kopańska¹, Andzelika Najda, Justyna Zebrowska, Lidia Chomicz, Janusz Piekarczyk, Przemysław Myjak, Maria Bretner

Affiliation

¹ Institute of Biochemistry and Biophysics, Polish Academy of Sciences, 5a Pawińskiego, 02-106 Warsaw, Poland.

PMID: 15110843
DOI: 10.1016/j.bmc.2004.03.022

Abstract

Chloro-, bromo- and methyl- analogues of 1H-benzimidazole and 1H-benzotriazole and their N-alkyl derivatives have been synthesized and tested in vitro against the protozoa Acanthamoeba castellanii. The results indicate that 5,6-dimethyl-1H-benzotriazole (11) and 5,6-dibromo-1H-benzotriazole (14) have higher efficacy than the antiprotozoal agent chlorohexidine.

MeSH terms

Acanthamoeba / drug effects*
Amebicides / chemical synthesis*
Amebicides / chemistry
Amebicides / pharmacology*
Animals
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Molecular Structure
Triazoles / chemistry
Triazoles / pharmacology*

Substances

Amebicides
Benzimidazoles
Triazoles
benzotriazole
benzimidazole