ArticleAntimicrobial agents and chemotherapy1998
Anti-Pneumocystis activities of aromatic diamidoxime prodrugs.
Article in Antimicrobial agents and chemotherapy, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 71 citations in OpenAlex.
- Oximes: Novel Therapeutics with Anticancer and Anti-Inflammatory Potential.Biomolecules · 2021Review
- Amidoximes and Oximes: Synthesis, Structure, and Their Key Role as NO Donors.Molecules (Basel, Switzerland) · 2019Review
- Quantitative analysis of amphiphilicChemicke zvesti · 2017Article
- The mammalian molybdenum enzymes of mARC.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2015Review
- Design and synthesis of N¹,N⁵-bis[4-(5-alkyl-1,2,4-oxadiazol-3-yl)phenyl]glutaramides as potential antifungal prodrugs.Molecules (Basel, Switzerland) · 2013Article
- Small-molecule binding to the DNA minor groove is mediated by a conserved water cluster.Journal of the American Chemical Society · 2013Article
- 2-(4-Amino-phen-yl)-3,4,5,6-tetra-hydro-pyrimidin-1-ium chloride.Acta crystallographica. Section E, Structure reports online · 2012Article
- Pharmacology of DB844, an orally active aza analogue of pafuramidine, in a monkey model of second stage human African trypanosomiasis.PLoS neglected tropical diseases · 2012Article
- Water-mediated binding of agents that target the DNA minor groove.Journal of the American Chemical Society · 2011Article
- Combined treatment of heterocyclic analogues and benznidazole upon Trypanosoma cruzi in vivo.PloS one · 2011Article
- Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.Antimicrobial agents and chemotherapy · 2010Article
- Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.Antimicrobial agents and chemotherapy · 2009Article
- (E)-1,1'-Bis[(E)-but-2-en-yl]-3,3'-(propane-1,3-di-yl)bis-(1H-benzimidazol-3-ium) dibromide monohydrate.Acta crystallographica. Section E, Structure reports online · 2008Article
- Antiparasitic compounds that target DNA.Biochimie · 2008Review
- Human African trypanosomiasis: pharmacological re-engagement with a neglected disease.British journal of pharmacology · 2007Review
- 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
- Highly active anti-Pneumocystis carinii compounds in a library of novel piperazine-linked bisbenzamidines and related compounds.Antimicrobial agents and chemotherapy · 2004Article
- Antifungal activity of some bis-5-methylbenzimidazole compounds.Folia microbiologica · 2003Article
- Immunoassays for pentamidine and related compounds: development of a facile inhibitory ELISA suitable for clinical use.Journal of clinical laboratory analysis · 2000Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Aromatic dicationic compounds, such as pentamidine, have potent antimicrobial activities. Clinical use of these compounds has been restricted, however, by their toxicity and limited oral activity. A novel approach, using amidoxime derivatives as prodrugs, has recently been proposed to overcome these limitations. Although results were presented for amidoxime derivatives of only one diamidine, pentamidine, the authors in the original proposal claimed that amidoxime derivatives would work as effective prodrugs for all pharmacologically active diamidines. Nine novel amidoxime derivatives were synthesized and tested in the present study for activity against Pneumocystis carinii in corticosteroid-suppressed rats. Only three of the nine compounds had significant oral anti-Pneumocystis activity. The bisbenzamidoxime derivatives of three direct pentamidine analogs had excellent oral and intravenous activities and reduced acute host toxicity. These compounds are not likely candidates for future drug development, however, because they have chronic toxic effects and the active amidine compounds have multiple sites susceptible to oxidative metabolism, which complicates their pharmacology and toxicology. Novel diamidoximes from three other structural classes, containing different groups linking the cationic moieties, lacked significant oral or intravenous anti-Pneumocystis activity, even though the corresponding diamidines were very active intravenously. Both active and inactive amidoximes were readily metabolized to the corresponding amidines by cell-free liver homogenates. Thus, the amidoxime prodrug approach may provide a strategy to exploit the potent antimicrobial and other pharmacological activities of selected, but certainly not all, aromatic diamidines.
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