151383-75-4

Upstream product

• 87-48-9 5-Bromo-1H-indole-2,3-dione 
• 3958-60-9 2-nitrophenylmethyl bromide 
• 66475-83-0 N-(4-bromophenyl)-2-(hydroxyimino) acetamide 
• 106-40-1 4-bromo-aniline 
• 88-72-2 1-methyl-2-nitrobenzene 
• 151383-63-0 N-(o-nitrobenzyl)-oxanilic acid 
• 33331-19-0 N-(2-nitrobenzyl)aniline 
• 151383-69-6 1-(2-Nitro-benzyl)-1H-indole-2,3-dione 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease

With the recent research advances in molecular biology and technology, multiple credible hypotheses about the progress of Alzheimer's disease (AD) have been proposed; multi-target drugs have emerged as an innovative therapeutic approach for AD. Current clinical therapy for AD patients is mainly palliative treatment targeting acetylcholinesterase (AChE). Inhibition of phosphodiesterase 5A (PDE5A) has recently been validated as a potentially novel therapeutic approach for Alzheimer's disease (AD). In this work, series of new compounds were designed, synthesized and evaluated as dual cholinesterase and PDE5A inhibitor. Biological results revealed that some of these compounds display good biological activities against AChE with IC50 values about 44.67–169.80 nM (donepezil IC50 50.12 nM). Notably, compound 12 presented potent activities against PDE5A with IC50 values about 50 μM (sildenafil IC50 12.59 μM), and some of these compounds showed low cell toxicity to A549 cells in vitro.

2-Indolone derivatives and open-ring derivatives, and synthetic methods and use thereof

The invention discloses 2-indolone derivatives and open-ring derivatives thereof, and synthetic method and a use thereof, belongs to the technical field of medicines, and relates to 2-indolone derivatives with the structure represented by general formula (I), and open-ring derivatives (II) thereof. In the formula (I) and formula (II), X is CO(CH2)n-1 and n is 1 to 10, or X is CO(CH2)n-1NH2 and n is 1 to 10; Y is CO or CH2; and R1, R2, R3, R4, R5, R6, R7 and R8 are different substituent groups. The invention also discloses structures, the synthetic methods and an in-vitro acetylcholinesterase and phosphodiesterase 5 inhibition activity, and can be further developed into new medicines for treating the Alzheimer's disease.

Synthesis and antimicrobial activity of some new indolo[2,1-b]quinazolin-6(12H)ones

A series of indolo[2,1-b]quinazolin-6(12H)ones 4a-i was prepared and tested for the antimicrobial activity. The synthesis of the new compounds and the results of the antimicrobial screening are reported.