36716-44-6

Upstream product

• 123-75-1 pyrrolidine 
• 935-06-8 N-(2-chloroethyl)aniline 
• 5050-41-9 N-(2-chloroethyl)-pyrrolidine 
• 62-53-3 aniline 
• 7154-73-6 1-(2-aminoethyl)pyrrolidine 
• 591-50-4 iodobenzene 
• 703-56-0 N-phenyl-2-oxazolidinone 

Downstream Products

• 101353-80-4 N-phenyl-N-(2-pyrrolidin-1-yl-ethyl)-propionamide 
• 100875-31-8 N-(2-pyrrolidino-ethyl)-acetanilide 
• 493-80-1 N-benzyl-N-(2-(pyrrolidin-1-yl)ethyl)aniline 
• 102164-01-2 N-(2-pyrrolidino-ethyl)-benzanilide 
• 130719-56-1 3-(4-Chlorphenyl)-4-phenyl-5-(2-pyrrolidinoethylanilino)isoxazol 
• 130719-60-7 3-(4-Chlorphenyl)-5-(2-pyrrolidinoethylanilino)isoxazol 

Relevant academic research and scientific papers

LIM KINASE INHIBITORS

A dynamic actin cytoskeleton is necessary for viral entry, intracellular migration, and virion release. For the human immunodeficiency virus (HIV), during viral entry, the virus triggers early actin activity through hijacking chemokine coreceptor signalin

Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors

The discovery/optimization of bis-aryl ureas as Limk inhibitors to obtain high potency and selectivity and appropriate pharmacokinetic properties through systematic SAR studies is reported. Docking studies supported the observed SAR. Optimized Limk inhibitors had high biochemical potency (IC50 400-fold), potent inhibition of cofilin phosphorylation in A7r5, PC-3, and CEM-SS T cells (IC50 1 μM), and good in vitro and in vivo pharmacokinetic properties. In the profiling against a panel of 61 kinases, compound 18b at 1 μM inhibited only Limk1 and STK16 with ≥80% inhibition. Compounds 18b and 18f were highly efficient in inhibiting cell-invasion/migration in PC-3 cells. In addition, compound 18w was demonstrated to be effective on reducing intraocular pressure (IOP) on rat eyes. Taken together, these data demonstrated that we had developed a novel class of bis-aryl urea derived potent and selective Limk inhibitors.

Short and practical synthesis of N′,N′-disubstituted N-aryl-1,2-ethylene-diamines by a decarboxylative ring-opening reaction under nucleophilic conditions

A straightforward and practical synthesis of N′,N′- disubstituted N-aryl-1,2-ethylenediamines, starting from anilines, via N-aryloxazolidin-2-ones is described. A decarboxylative ring-opening reaction of N-aryloxazolidin-2-ones, using aliphatic secondary