ArticleEuropean journal of medicinal chemistry2012
Analogs of pentamidine as potential anti-Pneumocystis chemotherapeutics.
Article in European journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 16 citations in OpenAlex.
- Characterization of theAntimicrobial agents and chemotherapy · 2024Article
- Structure-Activity Studies with Bis-Amidines That Potentiate Gram-Positive Specific Antibiotics against Gram-Negative Pathogens.ACS infectious diseases · 2021Article
- Drug-likeness of linear pentamidine analogues and their impact on the hERG KRSC advances · 2019Article
- Chloroquine Analogues as Leads against Pneumocystis Lung Pathogens.Antimicrobial agents and chemotherapy · 2018Article
- Phenotypic diversity and drug susceptibility of Trypanosoma cruzi TcV clinical isolates.PloS one · 2018Article
- Development of highly active anti-MedChemComm · 2017Article
- Article
- Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.Bioorganic & medicinal chemistry · 2015Article
- Probing the relationship between anti-Pneumocystis carinii activity and DNA binding of bisamidines by molecular dynamics simulations.Molecules (Basel, Switzerland) · 2015Article
- Diamidines versus Monoamidines as Anti-Pneumocystis Agents: An in Vivo Study.Pharmaceuticals (Basel, Switzerland) · 2013Article
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
A series of 20 pentamidine analogs were prepared using 2 general Schemes that evaluated heteroatoms, sulfobenzene and alkanediamide groups in the aliphatic linker and methoxy substituents attached to the benzene rings for efficacy against the fungal pathogen, Pneumocystis carinii in an ATP bioassay. All but one of the 20 bisamidines reduced the ATP content of the P. carinii over the 72 h of the assay period. The highest activities were associated with the lack of methoxy groups and the presence of the O, N and S heteroatoms. Activity (IC(50)) for compounds 1, 5, 6, 10 ranged from 1.1 to 2.13 μM. The compound 11 with similar activity (1.33 μM), bears a sulfobenzene group at a nitrogen in the aliphatic linker. The alkanediamide-linked bisbenzamidines showed a moderate inhibition of ATP. Generally, the inclusion of a heteroatom in the aliphatic linker and absence of methoxy groups at the benzene rings were associated with higher activities in this assay. Of note, most of the compounds had little to no cytotoxicity in mammalian cell cultures. Although not quite as potent as other pentamidine derivatives, these compounds hold promise for decreased side effects within the mammalian host.
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