35727-06-1

Upstream product

• 110-91-8 morpholine 
• 1516-60-5 4-nitrophenyl azide 
• 106-96-7 propargyl bromide 
• 90886-87-6 1‐(4‐nitrophenyl)‐1H‐1,2,3‐triazole‐4‐yl‐methanol 
• 1338831-20-1 (1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)methyl 4-methylbenzene-1-sulfonate 
• 100-01-6 4-nitro-aniline 
• 74820-13-6 4,5-dihydro-4-methylene-1-(4-nitrophenyl)-5-piperidino-1,2,3-triazole 
• 35726-98-8 4-[5-morpholin-4-ylmethyl-3-(4-nitro-phenyl)-4,5-dihydro-3H-[1,2,3]triazol-4-yl]-morpholine 

Relevant academic research and scientific papers

PVC-supported ethylenediamine-copper(II) complex: a heterogeneous, efficient, and eco-friendly catalyst for multi-component synthesis of 1,2,3-triazoles by reaction of propargyl bromide, aromatic azides, and amines in water

The PVC-supported ethylenediamine-copper(II) complex (PVC–EDA–Cu+2) has provided a highly efficient, active, and reusable heterogeneous catalyst for click chemistry. In this work, the PVC–EDA–Cu+2 catalyst is readily prepared by the

DDX3X inhibitors, an effective way to overcome HIV-1 resistance targeting host proteins

The huge resources that had gone into Human Immunodeficiency virus (HIV) research led to the development of potent antivirals able to suppress viral load in the majority of treated patients, thus dramatically increasing the life expectancy of people living with HIV. However, life-long treatments could result in the emergence of drug-resistant viruses that can progressively reduce the number of therapeutic options, facilitating the progression of the disease. In this scenario, we previously demonstrated that inhibitors of the human DDX3X helicase can represent an innovative approach for the simultaneous treatment of HIV and other viral infections such as Hepatitis c virus (HCV). We reported herein 6b, a novel DDX3X inhibitor that thanks to its distinct target of action is effective against HIV-1 strains resistant to currently approved drugs. Its improved in vitro ADME properties allowed us to perform preliminary in vivo studies in mice, which highlighted optimal biocompatibility and an improved bioavailability. These results represent a significant advancement in the development of DDX3X inhibitors as a novel class of broad spectrum and safe anti-HIV-1 drugs.

HUMAN HELICASE DDX3 INHIBITORS AS THERAPEUTIC AGENTS

The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.

General synthesis of (1-substituted-1H-1,2,3-triazol-4-ylmethyl)- dialkylamines via a copper(I)-catalyzed three-component reaction in water

A copper(I)-catalyzed three-component reaction to form (1-substituted-1H-1, 2,3-triazol-4-ylmethyl)-dialkylamines based on the Huisgen cycloaddition using amine, propargyl halide and azide in water was proposed. The process showed considerable synthetic advantages in terms of high atom economy, low environmental impact, atmospheric oxygen, wide substrate scope, mild reaction condition and good yields.