Synthesis, antiprotozoal and antibacterial activity of nitro- and halogeno-substituted benzimidazole derivatives.
Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-substituted modified benzimidazoles. Antibacterial and antiprotozoal activity of the newly obtained compounds was studied. Some thioalkyl derivatives showed remarkable activity against nosocomial strains of Stenotrophomonas malthophilia, and an activity comparable to that of metronidazole against gram-positive and gram-negative bacteria. Of the tested compounds, 5,6-dichloro-2-(4-nitrobenzylthio)-benzimidazole showed the most distinct antiprotozoal activity.
Institute of Chemistry, Agricultural University, Warszawa, Poland. kazimierczuk@delta.sggw.waw.pl
Zygmunt
Z
Kazimierczuk
Jacqueline A
JA
Upcroft
Peter
P
Upcroft
Agata
A
Górska
Bohdan
B
Starościak
Agnieszka
A
Laudy
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001562:Benzimidazoles / Q000138:chemical synthesis*; D056890:Eukaryota / Q000187:drug effects; D006219:Halogens / Q000378:metabolism
D000981:Antiprotozoal Agents; D001562:Benzimidazoles; D006219:Halogens; C031000:benzimidazole