ArticleBioorganic & medicinal chemistry letters2009
Synthesis and SAR of alkanediamide-linked bisbenzamidines with anti-trypanosomal and anti-pneumocystis activity.
Article in Bioorganic & medicinal chemistry letters, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria.RSC medicinal chemistry · 2022Article
- A Short Peptide Inhibitor as an Activity-Based Probe for Matriptase-2.Pharmaceuticals (Basel, Switzerland) · 2018Article
- Development of highly active anti-MedChemComm · 2017Article
- Alkanediamide-Linked Bisbenzamidines Are Promising Antiparasitic Agents.Pharmaceuticals (Basel, Switzerland) · 2016Article
- 3,1-Benzothiazines, 1,4-Benzodioxines and 1,4-Benzoxazines as Inhibitors of Matriptase-2: Outcome of a Focused Screening Approach.Pharmaceuticals (Basel, Switzerland) · 2016Article
- 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
- Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.Chemical reviews · 2014Review
- Structural aspects of intermolecular interactions in the solid state of 1,4-dibenzylpiperazines bearing nitrile or amidine groups.Acta crystallographica Section B, Structural science, crystal engineering and materials · 2014Article
- Activity of diimidazoline amides against African trypanosomiasis.Bioorganic & medicinal chemistry letters · 2014Article
- 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
- Diamidines versus Monoamidines as Anti-Pneumocystis Agents: An in Vivo Study.Pharmaceuticals (Basel, Switzerland) · 2013Article
- Analogs of pentamidine as potential anti-Pneumocystis chemotherapeutics.European journal of medicinal chemistry · 2012Article
- Bisbenzamidines as antifungal agents. are both amidine functions required to observe an anti-Pneumocystis carinii activity?Molecules (Basel, Switzerland) · 2010Article
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10 authors.
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Abstract
A series of alkanediamide-linked bisbenzamidines was synthesized and tested in vitro against a drug-sensitive strain of Trypanosoma brucei brucei, a drug-resistant strain of Trypanosoma brucei rhodesiense and Pneumocystiscarinii. Bisbenzamidines linked with longer alkanediamide chains were potent inhibitors of both strains of T. brucei. However, bisbenzamidines linked with shorter alkanediamide chains were the most potent compounds against P. carinii. N,N'-Bis[4-(aminoiminomethyl)phenyl] hexanediamide, 4 displayed potent inhibition (IC50=2-3 nM) against T. brucei and P. carinii, and was non-cytotoxic in the A549 human lung carcinoma cell line. The inhibitory bioactivity was significantly reduced when the amidine groups in 4 were moved from the para to the meta positions or replaced with amides.
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