274926-28-2

Upstream product

• 89-63-4 4-Chloro-2-nitroaniline 
• 5446-05-9 4-chloro-2-nitroiodobenzene 
• 274926-25-9 N-(5-chloro-2-iodo-phenyl)-N-(4-methoxybenzyl)-malonamic acid 
• 274926-24-8 N-(5-chloro-2-iodo-phenyl)-N-(4-methoxybenzyl)-malonamic acid methyl ester 
• 274926-23-7 (5-chloro-2-iodo-phenyl)-(4-methoxybenzyl)-amine 
• 824-94-2 p-methoxybenzyl chloride 
• 6828-35-9 5-chloro-2-iodoaniline 
• 274926-27-1 (E)-2-[(5-chloro-2-iodo-phenyl)-(4-methoxybenzyl)-carbamoyl]-5-phenylcarbamoyl-pent-4-enoic acid tert-butyl ester 
• 274926-26-0 N-(5-chloro-2-iodo-phenyl)-N-(4-methoxybenzyl)-malonamic acid tert-butyl ester 

Downstream Products

• 671207-69-5 (E)-8-chloro-2-oxo-5-phenylcarbamoylmethylene-2,3,4,5-tetrahydro-1H-benzo[b]azepine-3-carboxylic acid amide 
• 671207-75-3 (E)-2-[3-benzenesulfonylaminocarbonyl-8-chloro-1-(4-methoxy-benzyl)-2-oxo-1,2,3,4-tetrahydro-benzo[b]azepin-5-ylidene]-N-phenyl-acetamide 
• 671207-74-2 (E)-8-chloro-1-(4-methoxy-benzyl)-2-oxo-5-phenylcarbamoylmethylene-2,3,4,5-tetrahydro-1H-benzo[b]azepine-3-carboxylic acid 
• 671207-67-3 (E)-8-chloro-2-oxo-5-phenylcarbamoylmethylene-1,2,3,4-tetrahydro-1H-benzo[b]azepine-3-carboxylic acid 

Relevant academic research and scientific papers

Benzoazepine derivative as potent antagonists of the glycine binding site associated to the NMDA receptor

A series of benzoazepine derivatives, bearing suitable substituents at the C-3 position, was designed and evaluated by superimposition with the pharmacophore model of the glycine binding site. To fully explore the SAR of this class of compounds and to allow the preparation of new different compounds at the C-3 position, appropriate synthetic routes were set up. The benzoazepines were evaluated in terms of in vitro affinity using [ 3H]glycine binding assay and in vivo potency by inhibition of convulsions induced by N-methyl-D-aspartate (NMDA) in mice. This further analysis confirmed the preliminary results previously reported and that compound 27 is the most promising compound (Ki=32 nM, ED50=0.09 mg/kg, i.v.) in this series. Significant neuroprotective effect was observed after both pre- and post-ischaemia administration in the MCAo model. In particular, after post-ischaemia administration, it was found to be still effective when the administration was delayed up to 6 h after occlusion of the middle cerebral artery.

Synthesis and pharmacological properties of novel glycine antagonists

The NMDA receptor is an ionotropic receptor complex widely distributed in the central nervous system and its activation, particularly in hypoxic conditions such as stroke, traumatic head injury and hypoglycemia, results in a massive influx of calcium ions