3940-81-6

Upstream product

• 118-41-2 Eudesmic acid 
• 4521-61-3 3,4,5-Trimethoxybenzoyl chloride 
• 88-74-4 2-nitro-aniline 

Downstream Products

• 1270965-92-8 2-oxo-2-{2-[(3,4,5-trimethoxybenzoyl)amino]anilino}-ethyl acetate 
• 404894-28-6 N-(3',4',5'-trimethoxybenzoyl)-1,2-phenylenediamine 
• 1270965-97-3 N-{2-[(2,2-dimethylpropanoyl)amino]-phenyl}-3,4,5-trimethoxybenzamide 
• 175714-45-1 2-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazole 
• 57710-78-8 (1H?1,2,3?benzotriazol?1?yl)(3,4,5?trimethoxyphenyl)methanone 

Relevant academic research and scientific papers

Synthesis of Structurally Diverse Benzotriazoles via Rapid Diazotization and Intramolecular Cyclization of 1,2-Aryldiamines

An operationally simple method has been developed for the preparation of N-unsubstituted benzotriazoles by diazotization and intramolecular cyclization of a wide range of 1,2-aryldiamines under mild conditions, using a polymer-supported nitrite reagent and p-tosic acid. The functional group tolerance of this approach was further demonstrated with effective activation and cyclization of N-alkyl, -aryl, and -acyl ortho-aminoanilines leading to the synthesis of N1-substituted benzotriazoles. The synthetic utility of this one-pot heterocyclization process was exemplified with the preparation of a number of biologically and medicinally important benzotriazole scaffolds, including an α-amino acid analogue.

Benzimidazole compound and use thereof

The invention provides a benzimidazole compound and an application thereof. The compound has a structure shown in a formula (I). The compound is obtained by compound modification (namely respectively introducing R1 and R2) in site 1 and/or site 2 of 2-(3, 4, 5-trihydroxyl phenyl)-1H-benzimidazole. The benzimidazole compound provided by the invention can simulate Bim and competitively bind and antagonize Bcl-2/Mcl-1 protein in vitro and in cells so as to induce cell apoptosis, so that the benzimidazole compound is an apoptosis inducer and an anti-tumor compound with high activity.

Novel Mcl-1/Bcl-2 dual inhibitors created by the structure-based hybridization of drug-divided building blocks and a fragment deconstructed from a known two-face BH3 mimetic

We have previously reported a small-molecule two-face Bim BH3 mimetic, 2,3-dihydroxy-6-(4-isopropylphenylthio)anthracene-9,10-dione (1). Herein, we linked a polyphenol fragment, which was deconstructed from compound 1, with a drug-derived building block g

A journey from benzanilides to dithiobenzanilides: Synthesis of selective spasmolytic compounds

A series of dithiobenzanilide derivatives was synthesized and each compound was evaluated for its ability to reduce KCl-induced contractions of smooth muscle preparations of the guinea pig. Starting from a recent publication describing benzanilide derivatives as antispasmodic agents, structure-activity guided synthesis was performed to obtain compounds with improved spasmolytic activity. First, compounds with two amide bonds were designed and second, both amide oxygens were replaced by two sp2 sulfur atoms resulting in dithiobenzanilide derivatives. The most potent antispasmodic dithiobenzanilide 19 showed improved activity with an IC50 value of 0.4 μM. Moreover, the study also demonstrated that these active compounds were able to antagonize the effect of spasmogens like acetylcholine and phenylephrine and that the activity is not mediated by activation of ATP-dependent potassium channels (KATP-channels) or inhibition of endothelial nitric oxide synthase (eNOS).

Synthesis and CNS-depressant profile of 3,4,5-trimethoxybenzoyl analogues

A series of 3,4,5-trimethoxybenzoyl analogues with varying electronic and stereochemical characteristics has been synthesized. Many of these compounds (4, 5, 9, 12, 15) showed appreciable potentiation of pentobarbitone-induced hypnosis. Several analogues (1, 5, 6, 11, 12, 15) exhibited marked reduction of spontaneous motor activity (SMA).