1268487-55-3

Upstream product

• 528-45-0 3,4-dinitrobenzoic acid 
• 231634-78-9 4-(hex-5-yn-1-yloxy)benzaldehyde 
• 1268487-53-1 2-(4-(hex-5-ynyloxy)phenyl)-N-methoxy-N-methyl-3H-benzoimidazole-5-carboxamide 
• 660432-02-0 N-methoxy N-methyl 3,4-diaminobenzoic acid amide 
• 391903-19-8 N-methoxy N-methyl 3,4-dinitrobenzoic acid amide 

Downstream Products

• 1268487-57-5 2'-(4-(hex-5-ynyloxy)phenyl)-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzo[d]imidazole 

Relevant academic research and scientific papers

Selective Inhibition of Escherichia coli RNA and DNA Topoisomerase i by Hoechst 33258 Derived Mono-and Bisbenzimidazoles

A series of Hoechst 33258 based mono-and bisbenzimidazoles have been synthesized and their Escherichia coli DNA topoisomerase I inhibition, binding to B-DNA duplex, and antibacterial activity has been evaluated. Bisbenzimidazoles with alkynyl side chains display excellent E. coli DNA topoisomerase I inhibition properties with IC50 values 32 μg/mL). Bisbenzimidazoles showed varied stabilization of B-DNA duplex (1.2?ê'23.4 °C), and cytotoxicity studies show similar variation dependent upon the side chain length. Modeling studies suggest critical interactions between the inhibitor side chain and amino acids of the active site of DNA topoisomerase I.

Methods and compositions related to viral inhibition

Disclosed herein are compounds, compositions and methods related to viral inhibition. In some forms, the compounds, compositions and methods are related to binding RNA.

SELECTIVE INHIBITION OF BACTERIAL TOPOISOMERASE I

The present invention provides novel bisbenzimidazole compounds and methods of using the compounds as antibacterial agents.

Selective inhibition of bacterial topoisomerase i by alkynyl- bisbenzimidazoles

Hoechst dyes are well known DNA binders that non-selectively inhibit the function of mammalian topoisomerase I and II. Herein, we show that Hoechst 33258 based bisbenzimidazoles (DPA 151-154), containing a terminal alkyne, are effective and selective inhibitors of E. coli topoisomerase I. These bisbenzimidazoles displayed topoisomerase I inhibition much better than Hoechst 33342 or Hoechst 33258 with IC50 values in the range of 2.47-6.63 μM. Bisbenzimidazoles DPA 151-154 also display selective inhibition of E. coli topoisomerase I over DNA gyrase and human topoisomerases I and II, and effectively inhibit bacterial growth.