165596-46-3Relevant academic research and scientific papers
Synthesis and in vitro activity of dicationic bis-benzimidazoles as a new class of anti-MRSA and anti-VRE agents
Hu, Laixing,Kully, Maureen L.,Boykin, David W.,Abood, Norman
scheme or table, p. 1292 - 1295 (2009/10/15)
A new class of novel bis-benzimidazole diamidine compounds have been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Anti-MRSA and anti-VRE activities of the most potent compound 1 were more act
Synthesis and structure-activity relationship of dicationic diaryl ethers as novel potent anti-MRSA and anti-VRE agents
Hu, Laixing,Kully, Maureen L.,Boykin, David W.,Abood, Norman
scheme or table, p. 4626 - 4629 (2010/04/29)
A series of dicationic diaryl ethers have been synthesized and evaluated for in vitro antibacterial activities, including drug resistant bacterial strains. Most of these compounds have shown potent antibacterial activities. Several compounds, such as pipe
Antifungal activity of dicationic molecules
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, (2008/06/13)
Methods of treating fungal infections comprise administering a therapeutically effective amount of a compound described by Formulas [(I)-(VI)]. Examples of fungal infections include Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Fusariu
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents
Hopkins, Katherine T.,Wilson, W. David,Bender, Brendan C.,McCurdy, Donald R.,Hall, James Edwin,Tidwell, Richard R.,Kumar, Arvind,Bajic, Miro,Boykin, David W.
, p. 3872 - 3878 (2007/10/03)
The syntheses of nine new derivatives of 2,5-bis[4-(N- alkylamidino)phenyl]furans with extended aromatic systems are reported. The interaction of these dicationic furans with poly(dA)*poly(dT) and with the duplex oligomers d(CGCGAATTCGCG)2 and d(GCGAATTCGC)2 was determined by T(m) measurement, and the effectiveness of these compounds against the immunosuppressed rat model of Pneumocystis carinii was evaluated. At a screening dose of 10 μmol/kg, 4 of the 12 amidino furans described here are more active than the parent compound 1. In general, extension of the aromatic system in the absence of a substitution of the amidino nitrogens resulted in higher affinity for DNA than the parent compound as judged by the larger ΔT(m) values and suggests enhanced van der Waals interactions in the amidino furan-DNA complex. Three of the compounds, 3, 5, and 11, yield cysts counts of less than 0.1% of control when administered at a dosage of 10 μmol/kg. Compound 3, which does not have an extended aromatic system, is the most active derivative. Although a direct correlation between anti-P. carinii activity and DNA binding affinity was not observed, all compounds which have significant activity have large ΔT(m) values.
