4791-20-2

Upstream product

• 92-54-6 4-phenyl-1-piperazine 
• 103-71-9 phenyl isocyanate 

Downstream Products

• 67-56-1 methanol 
• 92-54-6 4-phenyl-1-piperazine 
• 62-53-3 aniline 

Relevant academic research and scientific papers

Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma

Pancreatic ductal adenocarcinoma (PDAC) is a lethal malignancy that is extremely refractory to the therapeutic approaches that have been evaluated to date. Recently, it has been demonstrated that PDAC tumors are dependent upon a metabolic pathway involving aspartate aminotransferase 1, also known as glutamate-oxaloacetate transaminase 1 (GOT1), for the maintenance of redox homeostasis and sustained proliferation. As such, small molecule inhibitors targeting this metabolic pathway may provide a novel therapeutic approach for the treatment of this devastating disease. To this end, from a high throughput screen of ～800,000 molecules, 4-(1H-indol-4-yl)-N-phenylpiperazine-1-carboxamide was identified as an inhibitor of GOT1. Mouse pharmacokinetic studies revealed that potency, rather than inherent metabolic instability, would limit immediate cell- and rodent xenograft-based experiments aimed at validating this potential cancer metabolism-related target. Medicinal chemistry-based optimization resulted in the identification of multiple derivatives with >10-fold improvements in potency, as well as the identification of a tryptamine-based series of GOT1 inhibitors.

Antidepressant activity of carbamates and urea derivatives

Thirteen (13) compounds of N-phenyl-O-alkyl carbamates (1 and 3), N,N-diethyl-N′-alkyl/aryl/phenylpiperazinoureas (4-6, 8-12), N-phenyl-N′-phenylpiperazino/imidazoureas (2, 7), and N-ethyl-(N′- phenylpiperazino) thioureas 13 were synthesized and tested for their antidepressant-like activity in mice. It was found that compound N-phenyl-O-heptyl carbamate 1 and N-phenyl-N′-phenylpiperazinourea 2 showed 32.5 and 27.7% antidepressant activity in the forced swim test in mice, respectively. Considering other carbamates it was found that a decrease in alkyl chain length caused a marked decline in the antidepressant activity. Compounds 1-4 show even higher activities in the forced swim test than the standard phenelzine. Springer Science+Business Media, LLC 2011.

Solid-phase synthesis of unsymmetrical ureas through the use of Kenner safety-catch linker

A new strategy for the solid-phase synthesis of unsymmetrical ureas is described. Upon treatment of Kenner safety-catch linker with an isocyanate, followed by TMSCHN2 or iodoacetonitrile and an amine, the corresponding unsymmetrical ureas are released in solution.