66639-62-1

Upstream product

• 17626-40-3 4-cyano-1,2-phenylenediamine 
• 106307-00-0 2-methoxyethyl 4-hydroxybenzimidate hydrochloride 
• 767-00-0 4-cyanophenol 
• 123-08-0 4-hydroxy-benzaldehyde 

Downstream Products

• 67770-95-0 2-methoxyethyl 2-(4-hydroxyphenyl)-5⁽⁶⁾-benzimidazolecarboximidate dihydrochloride 
• 136491-85-5 2'-(4-Hydroxy-phenyl)-1H,1'H-[2,5']bibenzoimidazolyl-5-carboxylic acid (3-dimethylamino-propyl)-amide; hydrochloride 
• 129012-05-1 2-(4-hydroxyphenyl)-3H-benzoimidazole-5-carbaldehyde 
• 1612254-45-1 5-(4-ethylpiperazin-1-yl)-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-46-2 5-(4-propylpiperazin-1-yl)-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-48-4 5-(4-(2-N,N-dimethylaminoethylpiperazin-1-yl))-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-47-3 5-(4-(2-N-trifluoroacetylaminoethylpiperazin-1-yl))-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-49-5 5-(4-phenylpiperazin-1-yl)-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-50-8 5-(4-(2-cyanophenylpiperazin-1-yl))-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-51-9 5-(4-(4-fluorophenylpiperazin-1-yl))-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-52-0 5-(4-pyridylpiperazin-1-yl)-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-53-1 5-(4-(2-pyrimidyl)piperazin-1-yl)-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 
• 1612254-54-2 5-(4-(4-aminophenyl)piperazin-1-yl)-2-[2′-(4-hydroxyphenyl)-5′-benzimidazolyl]benzimidazole 

Relevant academic research and scientific papers

Synthesis and evaluation of antioxidant and antiproliferative activity of 2-arylbenzimidazoles

Three series of arylbenzimidazole derivatives 3–40, 45 have been simply synthesized and tested for their antioxidant capacity. The 2-arylbenzimidazoles were tested against various radicals by the DPPH, FRAP and ORAC tests and showed different activity pro

New quinoline-arylamidine hybrids: Synthesis, DNA/RNA binding and antitumor activity

Four series of new hybrid molecules with 7-chloroquinoline and arylamidine moieties joined through the rigid -O- (groups I (2a-g) and II (5a-g)) or flexible -NH-CH2-CH2-O- (groups III (8a-g) and IV (10a-g)) linker were synthesized, and their DNA/RNA binding properties and cytotoxic activity were tested, against several human cancer lines. The compounds and their interaction with DNA and RNA were studied by UV–Vis and CD spectroscopy. The obtained results showed that the binding affinity of the investigated compounds increases proportionally with the increase of the length and number of groups able to form hydrogen bonds with ds-polynucleotides. Improvement of binding was additionally achieved by reduction of the structural rigidity of the investigated compounds, new hybrid compounds preferentially bind to ctDNA. For most of them the DNA/RNA grooves are dominant binding sites, except for the compounds from group II for which intercalation in polyA-polyU was the dominant binding mode. The antiproliferative effects were tested by the MTT test on normal (MDCK1), carcinoma (HeLa and CaCo2) and leukemia cell lines (Raji and K462). The GI50 values for all investigated compounds ranged from 5 to more than 100 × 10?6 mol dm?3. Carcinoma cells were more resistant to the investigated compounds than leukemia cells. The most effective compounds against leukemia cell lines were from group IV (10a-g), with GI50 values ranging from of 5 and 35 × 10?6 mol dm?3. The cell cycle arrest was investigated by flow cytometry and the obtained results indicate that the selected compounds, 2d, 2e, 8a, 10d, 10e, and 10f, induce changes in the cell cycle of treated cells, but the cycle phase distribution varies between them. A significant decrease in the number of cells in S phase (p 0.001) was observed in all treated cells, but only 10d and 10f induce cell cycle arrest at G0/G1 phase, dominantly.

Synthesis and biological evaluation of novel bisbenzimidazoles as Escherichia coli topoisomerase IA inhibitors and potential antibacterial agents

Novel bisbenzimidazole inhibitors of bacterial type IA topoisomerase are of interest for the development of new antibacterial agents that are impacted by target-mediated cross resistance with fluoroquinolones. The present study demonstrates the successful synthesis and evaluation of bisbenzimidazole analogues as Escherichia coli topoisomerase IA inhibitors. 5-(4-Propylpiperazin- 1-yl)-2-[2′-(4-ethoxyphenyl)-5′-benzimidazolyl]benzimidazole (12b) showed significant relaxation inhibition activity against EcTopo 1A (IC 50 = 2 ± 0.005 μM) and a tendency to chelate metal ion. Interestingly, these compounds did not show significant inhibition of E. coli DNA gyrase and hTop 1 even up to 100 μM. Compound 12b has shown lowest MIC against E. coli strains among 24 compounds evaluated. The binding affinity constant and binding free energy of 12b with EcTopo 1A was observed 6.8 × 106 M-1 and -10.84 kcal mol-1 from isothermal titration calorimetry (ITC), respectively. In vivo mouse systemic infection and neutropenic thigh model experimental results confirmed the therapeutic efficacy of 12b, suggesting further development of this class of compounds as antibacterial agents.

2-substituted phenyl-benzimidazole antibacterial agents

The invention relates to benzimidazole antibacterial compounds of the Formula I: STR1 as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.

2--5(6)-BENZIMIDAZOLECARBOXAMIDES

Condensation of the dihydrochlorides of 2-methoxyethyl carboximidates with o-phenylenediamines gave the amides of bisbenzimidazolecarboxylic acids containing amino or carboxyl groups in the amide fragment.The obtained a