88422-83-7

Usage

Type

Chemical compound

Development

Synthetic compound

Pharmacological properties

Potential anti-inflammatory and analgesic properties

Therapeutic potential

Potential candidate for the development of new pharmaceuticals

Unique structure

Interesting for further research and potential therapeutic applications

Investigation

Has been studied for its potential as a therapeutic agent

Upstream product

• 6780-38-7 N-phthaloylglycine chloride 
• 85-44-9 phthalic anhydride 
• 13156-95-1 2-chloro-N-phenethylacetamide 
• 4702-13-0 N-phthaloylglycine 
• 64-04-0 phenethylamine 
• 88422-74-6 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-(2-phenylethyl)acetamide 

Downstream Products

• 908249-20-7 2-[(1S)-1,2,3,4-tetrahydroisoquinolin-1-ylmethyl]-2,3-dihydro-1H-isoindole-1,3-dione 
• 1432065-37-6 benzyl-(1S,2R)-2-[(1S)-1-[(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)methyl]-1,2,3,4-tetrahydroisoquinoline-2-carbonyl]cyclohexane-1-carboxylate 
• 1432500-66-7 (1S,2R)-2-[(1S)-1-[(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)methyl]-1,2,3,4-tetrahydroisoquinolin-2-carbonyl]cyclohexane-1-carboxylic acid 
• 1432065-33-2 C₂₆H₂₆N₂O₅ 
• 1432065-34-3 C₂₆H₂₆N₂O₅ 
• 1432065-35-4 C₂₆H₂₆N₂O₅ 
• 310451-86-6 2-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)-1H-isoindole-1,3(2H)-dione 
• 60567-63-7 (1,2,3,4-tetrahydroisoquinoline-1-yl)methylamine dihydrochloride 

Relevant academic research and scientific papers

Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities

Tetrazanbigen (TNBG) is a novel sterol isoquinoline derivative with poor water solubility and moderate inhibitory effects on human cancer cell lines via lipoapoptosis induction. Herein, we developed a series of novel TNBG analogues with improved water sol

Novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and preparation and application thereof

The invention provides a novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and a preparation method and application thereof, and belongs to the field of chemical medicines. The derivative is a compound as shown in a formula I, or a salt thereof, or a stereoisomer thereof. The compound is low in toxicity or basically non-toxic to normal cells, has an obvious inhibition effect to tumor cell lines, particularly has good lipid toxicity selectivity to tumor cells such as liver cancer, lung cancer and the like in vivo, and has an obvious inhibition effect; meanwhile, the compound can effectively activate SREBP1 and PPAR gamma, inhibit lipid transport MTTP, cause lipid aggregation in tumor cells and cause lipid toxicity of the tumor cells. The compound can be used for treating liver cancer, lung cancer and the like in a molecular targeting manner, is low in toxicity or even non-toxic, and has a good application prospect.

HETEROCYCLIC COMPOUNDS AND USE THEREOF

Disclosed are compounds of formula (I) below or pharmaceutically acceptable salts thereof: in which each of variables R1-R6, L, m, and n is defined herein. Also disclosed are a method for treating an opioid receptor-associated condit

HETEROCYCLIC COMPOUNDS AND USE THEREOF

Disclosed are compounds of formula (I) below or pharmaceutically acceptable salts thereof:in which each of variables R 1 -R 6 , L, m, and n is defined herein. Also disclosed are a method for treating an opioid receptor-associated condition with a compound

A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity

Inhibiting the protein-protein interaction (PPI) between the transcription factor Nrf2 and its repressor protein Keap1 has emerged as a promising strategy to target oxidative stress in diseases, including central nervous system (CNS) disorders. Numerous non-covalent small-molecule Keap1-Nrf2 PPI inhibitors have been reported to date, but many feature suboptimal physicochemical properties for permeating the blood-brain barrier, while others contain problematic structural moieties. Here, we present the first side-by-side assessment of all reported Keap1-Nrf2 PPI inhibitor classes using fluorescence polarization, thermal shift assay, and surface plasmon resonance - and further evaluate the compounds in an NQO1 induction cell assay and in counter tests for nonspecific activities. Surprisingly, half of the compounds were inactive or deviated substantially from reported activities, while we confirm the cross-assay activities for others. Through this study, we have identified the most promising Keap1-Nrf2 inhibitors that can serve as pharmacological probes or starting points for developing CNS-active Keap1 inhibitors.

DIRECT INHIBITORS OF KEAP1-NRF2 INTERACTION AS ANTIOXIDANT INFLAMMATION MODULATORS

A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.

Pyridinopyrazine compounds and preparation method thereof, and medical application of pyridinopyrazine compounds

The invention relates to the field of pharmaceutical chemistry, particularly a series of pyridinopyrazine compounds (I). The pharmacodynamical test proves that the compounds are used for resisting external oxidation and electrophilic stimulation by activa

Synthesis and biological evaluation of 1,2,3,4-tetrahydroisoquinolines derivatives as monoamine oxidase inhibitors for treatment of Alzheimer's and Parkinson's diseases

A series of 1,2,3,4-tetrahydroisoquinolines derivatives were synthesized and evaluated their inhibition effect on monoamine oxidase (MAO). The results of pharmacological test revealed that all the five compounds had certain monoamine oxidase inhibitory ac

3-aroylmethylene-2,3,6,7-tetrahydro-1 H -pyrazino[2,1- a ]isoquinolin-4(11b H)-ones as potent Nrf2/ARE inducers in human cancer cells and AOM-DSS treated mice

Nrf2-mediated activation of ARE regulates expression of cytoprotective enzymes against oxidative stress, inflammation, and carcinogenesis. We have discovered a novel structure (1) as an ARE inducer via luciferase reporter assay to screen the in-house data

DIRECT INHIBITORS OF KEAP1-NRF2 INTERACTION AS ANTIOXIDANT INFLAMMATION MODULATORS

A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keapl-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.