3925-93-7

Upstream product

• 93053-63-5 5-ethoxy-2-phenyl-1⁽³⁾H-benzimidazole 
• 98-88-4 benzoyl chloride 
• 102-51-2 4-methoxy-1,2-phenylenediamine 
• 69570-97-4 methyl 2-phenyl-1H-benzo[d]imidazole-6-carboxylate 
• 36692-49-6 Methyl 3,4-diaminobenzoate 
• 100-52-7 benzaldehyde 
• 96-96-8 4-methoxy-2-nitroaniline 
• 885-81-4 N-(4-ethoxy-2-nitrophenyl)acetamide 
• 616-86-4 2-nitro-4-ethoxyaniline 
• 1197-37-1 4-ethoxy-benzene-1,2-diamine 
• 79877-53-5 5-methoxy-2-phenyl-1H-benzimidazole 
• 903751-98-4 N-(2-amino-5-methoxyphenyl)benzamide 

Downstream Products

• 131336-29-3 4-Nitro-2-phenyl-1H-benzoimidazol-5-ol 
• 131336-27-1 5-Hydroxy-2-phenyl-1H-benzoimidazole-4-sulfonic acid 
• 131336-30-6 4,6-Dinitro-2-phenyl-1H-benzoimidazol-5-ol 
• 131336-31-7 4,6-Dinitro-2-(4-nitro-phenyl)-1H-benzoimidazol-5-ol 
• 1370000-07-9 C₁₈H₁₉N₃O 
• 893772-64-0 C₁₉H₂₁N₃O 
• 1370000-10-4 C₁₈H₁₉N₃O₂ 
• 1370000-13-7 C₁₉H₂₂N₄O 
• 1370000-09-1 C₁₇H₁₉N₃O 
• 1370000-11-5 C₂₅H₂₅N₃O 
• 1370000-12-6 C₁₆H₁₇N₃O 
• 1370000-08-0 C₁₉H₂₁N₃O 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles as inhibitors of ebola virus infection

Novel 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles were designed and synthesized as Ebola virus inhibitors. The proposed structures of the new prepared benzimidazole-piperidine hybrids were confirmed based on their spectral data and CHN analyses. The target compounds were screened in vitro for their anti-Ebola activity. Among tested molecules, compounds 26a (EC50=0.93 μM, SI = 10) and 25a (EC50=0.64 μM, SI = 20) were as potent as and more selective than Toremifene reference drug (EC50 = 0.38 μM, SI = 7) against cell line. Data suggests that the mechanism by which 25a and 26a block EBOV infection is through the inhibition of viral entry at the level of NPC1. Furthermore, a docking study revealed that several of the NPC1 amino acids that participate in binding to GP are involved in the binding of the most active compounds 25a and 26a. Finally, in silico ADME prediction indicates that 26a is an idealy drug-like candidate. Our results could enable the development of small molecule drug capable of inhibiting Ebola virus, especially at the viral entry step.

Method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions

The invention discloses a method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions. According to the method, glacial aceticacid is taken as a catalyst; at solvent-free room temperature conditions, physical grinding is adopted, reaction of 2-substituted arylamines (2-mercapto arylamine, 2-aminophenol, and o-phenylenediamine) and aromatic aldehydes is carried out using physical grinding. The method is friendly to the environment, is simple in operation, is safe, is low in cost, and is high in efficiency. Compared withthe prior art, the advantages are that: the method is suitable for a large amount of functional groups, yield is high, less by-product is generated, operation is simple, the method is safe, cost is low, and the method is friendly to the environment.

Method for catalytically synthesizing benzimidazole compound by organic protonic acid under condition of no solvent

The invention discloses a method for catalytically synthesizing a benzimidazole compound by organic protonic acid under the condition of no solvent. According to the method provided by the invention,high efficiency catalysis is carried out to rapidly prep

Benzofuran derivatives as anticancer inhibitors of mTOR signaling

A series of 32 derivatives and isosteres of the mTOR inhibitor 2 were synthesized and compared for their cytotoxicity in radioresistant SQ20B cancer cell line. Several of these compounds, in particular 30b, were significantly more cytotoxic than 2. Importantly, 30b was shown to block both mTORC1 and Akt signaling, suggesting insensitivity to the resistance associated to Akt overactivation observed with rapamycin derivatives currently used in clinic.

Synthesis, antioxidant, and antimicrobial evaluation of some 2-arylbenzimidazole derivatives

A series of 2-arylbenzimidazole derivatives (3a-3p and 4a-4i) were synthesized and evaluated as potential antioxidant and antimicrobial agents. Their antioxidant properties were evaluated by various in vitro assays including hydroxyl radical (HO) scavenging, superoxide radical anion (O2 -) scavenging, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, and ferric reducing antioxidant power. Results demonstrated that compounds with hydroxyl group at the 5-position of benzimidazole ring had a comparable or better antioxidant activity in comparison to standard antioxidant tert-butylhydroquinone (TBHQ). Markedly, compound 4h that showed the highest HO scavenging activity (EC50 = 46 μM) in vitro had a significant reduction of 2,2′-azobis(2-amidinopropane) dihydrochloride (AAPH)-induced intracellular oxidative stress and H2O2-induced cell death. In addition, these compounds showed moderate to good inhibitory activity against Staphylococcus aureus selectively at noncytotoxic concentrations.

A novel series of benzimidazole NR2B-selective NMDA receptor antagonists

A series of novel benzimidazoles are discussed as NR2B-selective N-methyl-d-aspartate (NMDA) receptor antagonists. High throughput screening (HTS) efforts identified a number of potent and selective NR2B antagonists such as 1. Exploration of the substituents around the core of this template identified a number of compounds with high potency for NR2B (pIC50 >7) and good selectivity against the NR2A subunit (pIC50 2+ and radioligand binding studies. These agents offer potential for the development of therapeutics for a range of nervous system disorders including chronic pain, neurodegeneration, migraine and major depression.

BASICITY AND STRUCTURE OF 5-HYDROXYBENZIMIDAZOLES IN NITROMETHANE

Examination of the acid-base properties of 5-hydroxybenzimidazoles has shown them to exist in nitromethane as the 5-hydroxy-tautomers.Substituents in the 2-position have a predominantly inductive effect on the basicity of the 3-nitrogen, rationalized as in other nitrogen heterocycles by the proximity of the substituents to the reaction center. Keywords: 5-hydroxybenzimidazole, its tautomers and derivatives; acid-base properties and the effect thereon of substituents; Taft and inductive constants.