85730-47-8

Upstream product

• 53645-95-7 2-bromo-5-phenyl-1,3,4-thiadiazole 
• 105-53-3 diethyl malonate 
• 2002-03-1 2-amino-5-phenyl-1,3,4-thiadiazole 
• 86738-35-4 2-(methylsulfonyl)-5-phenyl-1,3,4-thiadiazole 

Downstream Products

• 85730-46-7 2-(5-phenyl-1,3,4-thiadiazol-2-yl)acetic acid 
• 85730-50-3 (5-Phenyl-[1,3,4]thiadiazol-2-yl)-(2,2,2-trichloro-ethoxycarbonylamino)-acetic acid ethyl ester 
• 85730-58-1 (5-Phenyl-[1,3,4]thiadiazol-2-ylmethyl)-carbamic acid 2,2,2-trichloro-ethyl ester 
• 85730-48-9 ethyl α-oximino-2-phenyl-1,3,4-thiadiazol-5-ylacetate 
• 85730-49-0 ethyl α-amino-2-phenyl-1,3,4-thiadiazol-5-ylacetate 
• 18070-82-1 2-ethoxycarbonylmethyl-5-phenyl-1,3,4-thiadiazole 
• 85730-57-0 C-(5-Phenyl-[1,3,4]thiadiazol-2-yl)-methylamine 

Relevant academic research and scientific papers

Discovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators

The present study describes the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-ylacetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, we identified a tetrazole scaffold that shifts away from the previously reported urea-based scaffolds while remaining effective GIRK1/2 channel activators. In addition, we evaluated the compounds in Tier 1 DMPK assays and have identified a (3-methyl-1H-pyrazol-1-yl)tetrahydrothiophene-1,1-dioxide head group that imparts interesting and unexpected microsomal stability compared to previously-reported pyrazole head groups.

ON THE REACTIVITY OF HALO-1,3-AZOLES AND RELATED COMPOUNDS TOWARD AROMATIC SN2 SUBSTITUTION

Nucleophilic addition-elimination reactions of 2-methylsulfonyl-1,3-azoles with active methylene compounds were investigated in order to compare the reactivity of substrates.The order of oxazole > thiazole >> N-methylimidazole in the reactivity was exhibited clearly.Furthermore, in oxazole and thiazole series, the predominant reactivity of the 2-position over the 4- and 5-positions was indicated on the reaction with the carbanions generated from active methylene compounds.