73259-41-3

Upstream product

• 4857-04-9 2-chloromethyl-1H-benzimidazole 
• 104-94-9 4-methoxy-aniline 
• 95-54-5 1,2-diamino-benzene 

Downstream Products

• 1284268-82-1 dichloro((1H-benzimidazol-2-ylmethyl)-(4-methoxyl-phenyl)amine)platinum(II) monohydrate 

Relevant academic research and scientific papers

Exploring electronic structure, and substituent effect of some biologically active benzimidazole derivatives: Experimental insights and DFT calculations

A series of (1H-benzimidazol-2-ylmethyl)-N-(4-phenyl)amine derivatives incorporating different electron-donating and withdrawing groups (X = 4[sbnd]OCH3 (1), 4[sbnd]CH3 (2), H (3), 4[sbnd]Cl (4), and 4[sbnd]Br (5)) on the para-position of the phenyl substituent was prepared, characterized and screened for their potential antimicrobial activity against some microbes. The substituent effect on the spectroscopic data (vibrational modes and NMR resonances) is well established by fitting with the Hammett constant. The unsubstituted derivative 4 exhibited comparable activity (MIC = 0.26 μM) to the standard tetracycline (MIC = 0.18 μM) against Staphylococcus aureus. Introduction of a substituent to the phenyl ring led to diminishing of the antibacterial activity. The substituent effect on the electron structure of 1–5 was investigated by TDDFT calculations. The acid dissociation constants of the ionizable NH group correlate well with Kubota's σ? parameter (R2 = 0.9196). The solvatochromism behavior of 1–5, in solvents of different polarity and hydrogen-bond tendency, was investigated by linear solvation–energy relationship equation analysis. Correlation between various quantum chemical descriptors, and antibacterial activity was carried out to verify a structural activity relation for this series of benzimidazole derivatives.

Benzimidazole derivative, benzothiophene derivative as well as preparation method and application of benzoimidazole derivative and benzothiophene derivative

The invention provides a benzimidazole derivative and a benzothiophene derivative. The benzimidazole derivative and the benzothiophene derivative respectively have structures shown in a formula (I) and a formula (IV). Experimental results show that the benzimidazole derivative and the benzothiophene derivative provided by the invention have good anti-tumor activity and can be used for preparing related tumor disease treatment medicines.

Novel tertiary sulfonamide derivatives containing benzimidazole moiety as potent anti-gastric cancer agents: Design, synthesis and SAR studies

With the expectation to find out new anti-gastric cancer agents with high efficacy and selectivity, a series of novel tertiary sulfonamide derivatives were synthesized and the anti-cancer activity was studied in three selected cancer cell lines (MGC-803, PC-3, MCF-7) in vitro. Some of the synthesized compounds could significantly inhibit the proliferation of these tested cancer cells and were more potent than the positive control (5-Fu). The structure-activity relationship of tertiary sulfonamide derivatives was explored in this report. Among the tested compounds, compound 13g containing benzimidazole moiety showed the best anti-proliferation activities against MGC-803 cells (IC50 = 1.02 μM), HGC-27 cells (IC50 = 1.61 μM), SGC-7901 (IC50 = 2.30 μM) cells as well as the good selectivity between the cancer and normal cells. Cellular mechanism studies elucidated compound 13g inhibited the colony formation of gastric cancer cell lines. Meanwhile, compound 13g arrested cell cycle at G2/M phase and induced cell apoptosis. Mechanistically, compound 13g markedly decreased p-Akt and p-c-Raf expression, which revealed that compound 13g targeted gastric cancer cell lines via interfering with AKT/mTOR and RAS/Raf/MEK/ERK pathways. All the findings suggest that compound 13g might be a valuable lead compound for the anti-gastric cancer agents.

Wavelength-Dependent Control of the CO Release Kinetics of Manganese(I) Tricarbonyl PhotoCORMs with Benzimidazole Coligands

A series of photoactivatable CO-releasing molecules (PhotoCORMs) was prepared from manganese pentacarbonyl bromide and 1H-benzimidazol-2-ylmethyl-(N-phenyl)amine ligands (L) bearing different electron-donating and electron-withdrawing groups R = H, 4-CHs

In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives

A series of 2-methylaminobenzimidazole derivatives (1-11) were synthesized by the reaction of 2-(chloromethyl)-1H-benzimidazole derivatives with primary aromatic amines. All these compounds were characterized by IR, 1H NMR, 13C NMR,