1449478-57-2

Upstream product

• 2646-26-6 4-(4-bromophenyl)semicarbazide 
• 157327-43-0 tert-butyl 5-acetyl-4-hydroxy-3,6-dihydropyridine-1(2H)-carboxylate 
• 217807-98-2 4-morpholin-4-yl-3,6-dihydro-2H-pyridine-1-carboxylic acid ter-tbutyl ester 
• 1449478-41-4 C₁₄H₁₅BrN₄O 
• 75-03-6 ethyl iodide 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 

Relevant academic research and scientific papers

Discovery of novel tetrahydro-pyrazolo [4,3-c] pyridines for the treatment of neuropathic pain: Synthesis and neuropharmacology

We disclose the discovery of a novel series of tetrahydropyrido-pyrazoles that are potent inhibitors of tumour necrosis factor-alpha (TNF-α), nitric oxide and cannabinoid receptor subtype 1 (CB1). We report herein the synthesis and neuropharmacological screening results of the titled compounds in two acute pain and two neuropathic pain models in rodents. Particularly the analogue N-(4-bromophenyl)-3-tert-butyl-5-ethyl-4,5,6,7-tetrahydro-1H- pyrazolo[4,3-c]pyridine-1-carboxamide (8a) exhibited pronounced acute antinociceptive efficacy, also being effective in chronic constriction injury (ED50 = 23.8 mg/kg) and partial sciatic nerve injury (ED50 = 29.0 mg/kg) models with CB1 receptor activity (IC50 = 49.6 nM) and inhibitory effect on TNF-α (86.4% inhibition at 100 mg/kg). These results suggest the importance of the development of this lead as multi-targeted treatment strategy for neuropathic pain.