374889-98-2

Upstream product

• 399-31-5 N-(2-fluorophenyl)acetamide 
• 39184-82-2 N-(2-fluorophenyl)ethanethioamide 
• 374889-97-1 methyl N-(2-fluorophenyl)ethanimidothioate 
• 5933-32-4 4-bromobenzoic acid hydrazide 

Downstream Products

• 374886-60-9 3-{4-[4-(2-fluorophenyl)-5-methyl-4H-1,2,4-triazol-3-yl]-phenyl}pyridine 
• 374886-59-6 4-(2-Fluorophenyl)-3-methyl-5-(4-thiophen-2-ylphenyl)-4H-1,2,4-triazole 
• 374886-83-6 4-{4-[4-(2-fluorophenyl)-5-methyl-4H-1,2,4-triazol-3-yl]-phenyl}pyridine 

Relevant academic research and scientific papers

Atropisomeric 4-phenyl-4 H -1,2,4-triazoles as selective glycine transporter 1 inhibitors

We report on the optimization of 4H-1,2,4-triazole derivatives to increase their activity and selectivity as glycine transporter 1 (GlyT1) inhibitors. Structure-activity relationship exploration resulted in the identification of a 3-[3-ethyl-5-(6-phenylpyridin-3-yl)-4H-1,2,4-triazol-4-yl]-2-methylbenzonitrile (14u) compound with markedly higher selectivity for GlyT1. Physiochemical studies revealed that 14u exists as a stable pair of atropisomers under physiological conditions. We successfully separated the atropisomers to obtain active enantiomer (R)-14u, which displayed favorable pharmacokinetic properties, as well as positive results in the mice Y-maze test.

Triazole derivatives

The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.