ArticleAntimicrobial agents and chemotherapy1993
Structure-activity studies of dicationically substituted bis-benzimidazoles against Giardia lamblia: correlation of antigiardial activity with DNA binding affinity and giardial topoisomerase II inhibition.
Article in Antimicrobial agents and chemotherapy, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 94 citations in OpenAlex.
- Phase I/II evaluation of the prophylactic antimalarial activity of pafuramidine in healthy volunteers challenged with Plasmodium falciparum sporozoites.The American journal of tropical medicine and hygiene · 2009Trial
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- Marked antigiardial activity of Yucca baccata extracts: a potential natural alternative for treating protozoan infections.BioMed research international · 2014Article
- Phosphonoxins III: synthesis of α-aminophosphonate analogs of antifungal polyoxins with anti-Giardia activity.Organic letters · 2010Article
- Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.Journal of medicinal chemistry · 2010Article
- The Application of DNA-Biosensors and Differential Scanning Calorimetry to the Study of the DNA-Binding Agent Berenil.Sensors (Basel, Switzerland) · 2008Article
- CYP4F enzymes are the major enzymes in human liver microsomes that catalyze the O-demethylation of the antiparasitic prodrug DB289 [2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime].Drug metabolism and disposition: the biological fate of chemicals · 2006Article
- In vitro selection and in vivo efficacy of piperazine- and alkanediamide-linked bisbenzamidines against Pneumocystis pneumonia in mice.Antimicrobial agents and chemotherapy · 2006Article
- Evaluation of silymarin in the treatment on asymptomatic Giardia infections in dogs.Parasitology research · 2005Article
- Highly active anti-Pneumocystis carinii compounds in a library of novel piperazine-linked bisbenzamidines and related compounds.Antimicrobial agents and chemotherapy · 2004Article
- Characterization of a novel DNA minor-groove complex.Biophysical journal · 2004Article
- Molecular characterization of recombinant Pneumocystis carinii topoisomerase I: differential interactions with human topoisomerase I poisons and pentamidine.Antimicrobial agents and chemotherapy · 2002Article
- Induced fit DNA recognition by a minor groove binding analogue of Hoechst 33258: fluctuations in DNA A tract structure investigated by NMR and molecular dynamics simulations.Nucleic acids research · 2001Article
- Sequence-dependent variation in DNA minor groove width dictates orientational preference of Hoechst 33258 in A-tract recognition: solution NMR structure of the 2:1 complex with d(CTTTTGCAAAAG)(2).Nucleic acids research · 2000Article
- Comparative efficacy evaluation of dicationic carbazole compounds, nitazoxanide, and paromomycin against Cryptosporidium parvum infections in a neonatal mouse model.Antimicrobial agents and chemotherapy · 1998Article
- In vitro antifungal activities of a series of dication-substituted carbazoles, furans, and benzimidazoles.Antimicrobial agents and chemotherapy · 1998Article
- Structure-in vitro activity relationships of pentamidine analogues and dication-substituted bis-benzimidazoles as new antifungal agents.Antimicrobial agents and chemotherapy · 1998Article
- Anti-Pneumocystis activities of aromatic diamidoxime prodrugs.Antimicrobial agents and chemotherapy · 1998Article
- Anti-Pneumocystis carinii pneumonia activity of dicationic 2,4-diarylpyrimidines.European journal of medicinal chemistry · 1996Article
- Synthesis of dicationic diarylpyridines as nucleic-acid binding agents.European journal of medicinal chemistry · 1995Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Nine dicationically substituted bis-benzimidazoles were examined for their in vitro activities against Giardia lamblia WB (ATCC 30957). The potential mechanisms of action of these compounds were evaluated by investigating the relationship among in vitro antigiardial activity and the affinity of the molecules for DNA and their ability to inhibit the activity of giardial topoisomerase II. Each compound demonstrated antigiardial activity, as measured by assessing the incorporation of [methyl-3H]thymidine by giardial trophozoites exposed to the test agents. Three compounds exhibited excellent in vitro antigiardial activities, with 50% inhibitory concentrations which compared very favorably with those of two currently used drugs, quinacrine HCl and metronidazole. Putative mechanisms of action for these compounds were suggested by the strong correlation observed among in vitro antigiardial activity and the affinity of the molecules for natural and synthetic DNA and their ability to inhibit the relaxation activity of giardial topoisomerase II. A strong correlation between the DNA binding affinity of these compounds and their inhibition of giardial topoisomerase II activity was also observed.
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