97420-36-5

Upstream product

• 615-15-6 2-Methyl-1H-benzimidazole 
• 105-39-5 chloroacetic acid ethyl ester 
• 105-36-2 ethyl bromoacetate 

Downstream Products

• 131698-45-8 4-phenyl-1-[1-carbonylmethyl-(2-methyl-1H-benzimidazole)]-thiosemicarbazide 
• 131698-52-7 1-[(4-phenyl-3-thioxy-4H-1,2,4-triazol-5-yl)methyl]-2-methyl-1H-benzimidazoles 
• 343977-51-5 1-[(4-(4'-methylphenyl)-3-thioxy-4H-1,2,4-triazol-5-yl)methyl]-2-methyl-1H-benzimidazoles 
• 343977-52-6 1-[(4-(4'-chlorophenyl)-3-thioxy-4H-1,2,4-triazol-5-yl)methyl]-2-methyl-1H-benzimidazoles 
• 343977-49-1 4-(4'-methylphenyl)-1-[1-carbonylmethyl-(2-methyl-1H-benzimidazole)]-thiosemicarbazide 
• 343977-50-4 4-(4'-chlorophenyl)-1-[1-carbonylmethyl-(2-methyl-1H-benzimidazole)]-thiosemicarbazide 

Relevant academic research and scientific papers

COMPOSITIONS FOR TRANSFECTING A NUCLEIC ACID MOLECULE INTO A CELL COMPRISING HETEROCYCLIC COMPOUNDS GRAFTED TO A CATIONIC POLYMER, AND THEIR APPLICATIONS

The present invention relates to compositions for transfecting a nucleic acid molecule into a cell and their applications. The present invention is directed to a composition suitable for transfecting a nucleic acid molecule into a cell, preferably a eukaryotic cell, comprising (i) at least one compound of general formula (II) or a tautomer, mesomer, racemate, enantiomer, diastereomer, or mixture thereof, or an acceptable salt thereof, and (ii) an acceptable excipient, buffering agent, cell culture medium, or transfection medium, wherein Y11, Y22, Y33, Z11, Z22, Z33, Z44, Z55, Z66, Z77, X11, X22, R33, P++, R, T, U and V are as defined in the description. The present invention also relates to uses of said composition and to a method for in vitro or ex vivo transfection of live cells.

Dihydro quinazolinone derivative, as well as preparation method and application thereof

The invention relates to the technical field of medicines, in particular to a new dihydro quinazolinone derivative with the following chemical structure general formula and pharmaceutically acceptablesalts thereof, (the formula is shown in the description.), A pharmacological experiment shows that the derivative or the salt provided by the invention has higher inhibitory activity on KRAS-PDE delta protein interaction, and has higher anti-tumor activity in vitro. The invention also provides a preparation method of the derivative and the pharmaceutically acceptable salts thereof, and application to preparatioin of a KRAS-PDE delta inhibitor and an anti-tumor drug.

Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design

Targeting KRAS-PDEδ protein-protein interactions with small molecules represents a promising opportunity for developing novel antitumor agents. However, current KRAS-PDEδ inhibitors are limited by poor cellular antitumor potency and the druggability of the target remains to be validated by new inhibitors. To tackle these challenges, herein, novel, highly potent KRAS-PDEδ inhibitors were identified by fragment-based drug design, providing promising lead compounds or chemical probes for investigating the biological functions and druggability of KRAS-PDEδ interaction.

Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3β inhibitors with anti-depressant activity

A series of benzimidazole based thiadiazole and carbohydrazide conjugates have been synthesized and evaluated for inhibition of glycogen synthase kinase-3β and anti-depressant effect. Compounds 4f, 4j, 5b, 5g and 5i were found to be the most potent inhibitors of GSK-3β in vitro amongst the twenty-five benzimidazole based thiadiazole and carbohydrazide conjugates synthesized. Compound 5i was also found to exhibit significant antidepressant activity in vivo at 50?mg/kg, when compared to fluoxetine, a known antidepressant drug. The molecular docking studies revealed multiple hydrogen bond interactions by the synthesized compounds with various amino acid residues, viz, ASP-133, LYS-183, PRO-136, VAL-135, TYR-134, or LYS-60 at the GSK-3β receptor site.

Synthesis and Antibacterial Activity of Some Derivatives of 2-Methylbenzimidazole Containing 1,3,4-Oxadiazole or 1,2,4-Triazole Heterocycle

5-[(2-Methyl-1H-benzimidazol-1-yl)methyl]-1,3,4-oxadiazole-2-thiol or 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-4-(4-methylphenyl)-1,2,4-triazol-3-thiol which were prepared starting from 2-methylbenzimidazole in the reaction with appropriate N-aryl-2-chlo

Electroanalytical and computational studies on the corrosion inhibition behavior of ethyl (2-methylbenzimidazolyl) acetate (EMBA) on mild steel in hydrochloric acid

The interaction and corrosion protection properties of ethyl (2-methylbenzimidazolyl) acetate (EMBA) on mild steel in hydrochloric acid (0.5, 1 and 1.5 M) at different temperatures have been studied by polarization, EIS, adsorption, surface studies, and computational calculations. Polarization studies showed that this molecule act as mixed-type inhibitor. EMBA acts as an effective inhibitor for mild steel in hydrochloric acid at different temperatures (303, 308, and 313 K). At room temperature, EMBA was found to be a more effective inhibitor and its efficiency decreases with increasing temperature. The mechanism involves adsorption of inhibitor molecules on the metal surface and this process obeys the Langmuir isotherm.

Ultrasound promoted simple and efficient N-alkylation of 2-substituted benzimidazoles

N-Alkylation of 2-chlorobenzimidazole was carried out using different alkylating agents under ultrasound irradiation technique. These reactions were completed in shorter times and with higher percentage of yields. Among all the green solvents, triethanolamine was found to be very effective and also acts as a base. The above reaction conditions were extended to other 2-substituted benzimidazoles. Thus, a simple and efficient route for N-alkylation has been developed using ultrasound irradiation technique.

Synthesis and biological activity of some triazole-bearing benzimidazole derivatives

A number of N'-(arylmethylidene)-2-(2-methyl-1H-benzimidazol- -1-yl)acetohydrazide and 4-aryl-5-[(2-methyl-1H-benzimidazol-1-yl)methyl]- -4H-1,2,4-triazole-3-thiol derivatives were synthesized by incorporating various aromatic and heterocyclic substituents on 2-methyl-1H-benzimidazole. The structures of all the synthesized compounds were elucidated based on their elemental analyses and spectral data. The in vitro activities of these compounds against bacteria and fungi were evaluated by the disc diffusion and the minimum inhibitory concentration (MIC) methods. Some of the synthesized derivatives were found to be as active as kanamycin (standard drug).

Synthesis of novel 2,5-disubstituted 1,3,4-thiadiazoles: Structural requirements necessary for anticonvulsant activity

The synthesis of novel 2,5-disubstituted 1,3,4-thiadiazoles and their anticonvulsant activity was analyzed. The synthesis of 1-[5-{(2-methyl-1H- benzimidazol-1-yl)methyl}-1,3,4-thiadiazol-2-yl]-urea involved the dissolution of 5-[(2-methyl-1H-benzimidazol-1-yl)-methyl]-1,3,4-thiadiazol-2-amine in 10 ~ 30 mL of glacial acetic acid diluted to 50 mL with distilled water and to the equimolar (0.01 mol) quantity of sodium cyanate in 20 ~ 30 mL of warm water was added. The precipitates obtained were collected by filtration, washed with cold water and recrystallized from 90% aqueous ethanol. The synthesis of N-[5-(1H-indol-3-yl-methyl)-1,3,4-thiadiazol-2-yl]-hydrazinecarboxamide involved the dissolution of 1-[5-{(2-methyl-1H-benzimidazol-1-yl)methyl}-1,3,4- thiadiazol-2-yl]-urea in 30 ~ 40 mL and to the mixture equimolar solution of hydrazine hydrate in 5 mL of water was added. The product was filtered and recrystallized from 90% aqueous ethanol. It was reported that majority of the compounds exhibited anticonvulsant activity.

Synthesis and evaluation of some new benzimidazole derivatives as potential antimicrobial agents

The efficient synthesis of novel azetidin-2-ones 6 has been established. Thus, condensation of 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-1,3,4-thiadiazol-2-amine 4 with various aromatic aldehydes afforded 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-N-[(subs