1809031-84-2

Usage

Uses

Used in Medicinal Chemistry:
1-(3-iodophenyl)-4-(3-nitrophenyl)-1H-1,2,3-triazole is used as a compound with potential biological activity for the development of new drugs. Its triazole ring and substituted phenyl groups may contribute to its interaction with biological targets, making it a promising candidate for further research and development in the pharmaceutical industry.
Used in Chemical Modifications and Functionalizations:
1-(3-iodophenyl)-4-(3-nitrophenyl)-1H-1,2,3-triazole is used as a starting material for further chemical modifications and functionalizations. Its structure allows for the possibility of creating new compounds with enhanced properties or specific applications in various industries, such as materials science, agrochemicals, and more.

Upstream product

• 585-79-5 m-nitrobromobenzene 
• 645-00-1 m-iodonitrobenzene 

Relevant academic research and scientific papers

Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1-Nrf2 Protein-Protein Interaction

The transcription factor Nrf2 regulates the expression of a large network of cytoprotective and metabolic enzymes and proteins. Compounds that directly and reversibly inhibit the interaction between Nrf2 and its main negative regulator Keap1 are potential pharmacological agents for a range of disease types including neurodegenerative conditions and cancer. We describe the development of a series of 1,4-diphenyl-1,2,3-triazole compounds that inhibit the Nrf2-Keap1 protein-protein interaction (PPI) in vitro and in live cells and up-regulate the expression of Nrf2-dependent gene products.

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.