380653-35-0Relevant academic research and scientific papers
An easy and efficient protocol for the condensation reaction of isatin and N-substituted isatins with 1,2-diaminobenzene using low cost reusable clay catalyst
Bajpai, Shivam,Singh, Sundaram,Srivastava, Vandana
, p. 37 - 39 (2014)
A green procedure was developed for the condensation of isatin and N-substituted isatins with 1,2-diaminobenzene by using reusable bentonite clay in EtOH/H2O solvent system, under microwave irradiation. This eco-friendly synthesis is characterized by high yields and short reaction times. The catalyst is easily recycled.
Indoloquinoxaline derivatives as promising multi-functional anti-Alzheimer agents
Kanhed, Ashish M.,Patel, Dushyant V.,Patel, Nirav R.,Sinha, Anshuman,Thakor, Priyanka S.,Patel, Kishan B.,Prajapati, Navnit K.,Patel, Kirti V.,Yadav, Mange Ram
, p. 2498 - 2515 (2020/11/02)
To confront a disease like Alzheimer’s disease having complex pathogenesis, development of multitarget-directed ligands has emerged as a promising drug discovery approach. In our endeavor towards the development of multitarget-directed ligands for Alzheimer’s disease, a series of indoloquinoxaline derivatives were designed and synthesized. In vitro cholinesterase inhibition studies revealed that all the synthesized compounds exhibited moderate to good cholinesterase inhibitory activity. 6-(6-(Piperidin-1-yl)hexyl)-6H-indolo[2,3-b]quinoxaline 9f was identified as the most potent and selective BuChE inhibitor (IC50 = 0.96 μM, selectivity index = 0.17) that possessed 2 fold higher BuChE inhibitory activity compared to the commercially approved reference drug donepezil (IC50 = 1.87 μM). Moreover, compound 9f is also endowed with self-induced Aβ1-42 aggregation inhibitory activity (51.24% inhibition at 50 μM concentration). Some of the compounds of the series also displayed moderate anti-oxidant activity. To perceive a putative binding mode of the compound 9f, molecular docking studies were carried out, and the results pointed out significant interactions of compound 9f with the enzymes in the binding sites of cholinesterases as well as Aβ1-42. Additionally, compound 9f exhibited favorable in silico ADMET properties. Put together these findings project compound 9f as a potential multitarget-directed ligand in the direction of developing novel anti-AD drugs. Communicated by Ramaswamy H. Sarma.
One-step method for preparing indole quinoxaline compound
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Paragraph 0023-0026, (2019/10/10)
The invention relates to a synthetic method for preparing an indole quinoxaline compound. The method particularly comprises the following steps: adding an o-phenylenediamine compound, a diketone indoline compound, alkyl halide, acid, a fluorine oxidizer according to the molar ratio of1:1:1.2:0.2:0.2 into toluene, performing refluxing and quenching reaction to obtain a reaction mixture, extracting the reaction product, merging an organic phase, concentrating filtrate, and separating by column chromatography to obtain the indole quinoxaline compound. The method has the advantages that the reaction is completed by a onestep method, the problems of low roductivity yield and difficult reaction of a multi-step system are solved, and inert gas protection is not required, and the operation process is simplified. The method has broad application prospects in the aspects of natural products, medicines, pesticides, herbicides, the synthesis of organic photoelectric materials and liquid crystal materials and the like.
