313405-50-4

Upstream product

• 99-73-0 para-bromophenacyl bromide 
• 2103-94-8 4-(4-bromophenyl)-1,3-thiazol-2-amine 
• 4023-34-1 cyclopropanecarboxylic acid chloride 

Downstream Products

• 1426259-66-6 N-(4-{4-[2-(2-methoxyethoxy)pyridin-4-yl]phenyl}thiazol-2-yl)cyclopropanecarboxamide 
• 1426259-63-3 N-(4-{4-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]phenyl}thiazol-2-yl)cyclopropanecarboxamide 
• 1426259-69-9 N-(4-{4-[6-(2-methoxyethoxy)pyridin-3-yl]phenyl}thiazol-2-yl)cyclopropanecarboxamide 
• 1448015-71-1 N-{4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]thiazol-2-yl}cyclopropanecarboxamide 
• 1448015-74-4 C₁₈H₁₅N₃OS 
• 1448015-76-6 cyclopropanecarboxylic acid {4-[4-(2-methylpyridin-3-yl)phenyl]thiazol-2-yl}amide 
• 1448015-81-3 cyclopropanecarboxylic acid {4-[4-(2-methyl-2H-pyrazol-3-yl)-phenyl]thiazol-2-yl}amide 
• 1448015-84-6 cyclopropanecarboxylic acid {4-[4-(3,5-dimethylisoxazol-4-yl)-phenyl]thiazol-2-yl}amide 
• 1448015-78-8 cyclopropanecarboxylic acid {4-[4-(6-dimethylaminopyridin-3-yl)phenyl]thiazol-2-yl}amide 

Relevant academic research and scientific papers

2-Aminothiazoles with Improved Pharmacotherapeutic Properties for Treatment of Prion Disease

Recently, we described the aminothiazole lead (4-biphenyl-4-ylthiazol-2-yl)-(6-methylpyridin-2-yl)-amine (1), which exhibits many desirable properties, including excellent stability in liver microsomes, oral bioavailability of ～40%, and high exposure in the brains of mice. Despite its good pharmacokinetic properties, compound 1 exhibited only modest potency in mouse neuroblastoma cells overexpressing the disease-causing prion protein PrPSc. Accordingly, we sought to identify analogues of 1 with improved antiprion potency in ScN2a-cl3 cells while retaining similar or superior properties. Herein we report the discovery of improved lead compounds such as (6-methylpyridin-2-yl)-[4-(4-pyridin-3-yl-phenyl)thiazol-2-yl]amine and cyclopropanecarboxylic acid (4-biphenylthiazol-2-yl)amide, which exhibit brain exposure/EC50 ratios at least tenfold greater than that of compound 1.