27228-22-4

Upstream product

• 540-72-7 sodium thiocyanide 
• 34918-74-6 N-(4-methoxyphenyl)benzimidoyl chloride 
• 104-94-9 4-methoxy-aniline 
• 98-88-4 benzoyl chloride 
• 333-20-0 potassium thioacyanate 
• 7472-54-0 N-(p-methoxyphenyl)benzamide 

Downstream Products

• 75508-84-8 6-Fluoren-9-ylidene-1-(4-methoxy-phenyl)-2-phenyl-5-(triphenyl-λ⁵-phosphanylidene)-5,6-dihydro-1H-pyrimidine-4-thione 
• 75508-83-7 N-[4-Fluoren-9-ylidene-3-(triphenyl-λ⁵-phosphanylidene)-thietan-(2Z)-ylidene]-N'-(4-methoxy-phenyl)-benzamidine 
• 75509-03-4 N-(4-Methoxy-phenyl)-N'-[4-[(Z)-phenylimino]-3-(triphenyl-λ⁵-phosphanylidene)-thietan-(2Z)-ylidene]-benzamidine 
• 666175-17-3 1-ethyl-3-[(phenyl)-(4-methoxyphenylimino)methyl]thiourea 
• 1281681-04-6 1-ethoxycarbonylmethyl-3-(N-4-methoxyphenylbenzymidoyl)thiourea 
• 666175-09-3 1-methyl-3-[(phenyl)-(4-methoxyphenylimino)methyl]thiourea 
• 20800-67-3 N-(4-methoxy-phenyl)-N'-[1,2,3]thiadiazol-5-yl-benzamidine 

Relevant academic research and scientific papers

5-Imino-1,2,4-thiadiazoles: First small molecules As substrate competitive inhibitors of glycogen synthase kinase 3

Cumulative evidence strongly supports that glycogen synthase kinase-3 (GSK-3) is a pathogenic molecule when it is up-dysregulated, emerging as an important therapeutic target in severe unmet human diseases. GSK-3 specific inhibitors might be promising effective drugs for the treatment of devastating pathologies such as neurodegenerative diseases, stroke, and mood disorders. As GSK-3 has the ability to phosphorylate primed substrates, small molecules able to bind to this site should be perfect drug candidates, able to partially block the activity of the enzyme over some specific substrates. Here, we report substituted 5-imino-1,2,4-thiadiazoles as the first small molecules able to inhibit GSK-3 in a substrate competitive manner. These compounds are cell permeable, able to decrease inflammatory activation and to selectively differentiate neural stem cells. Overall, 5-imino-1,2,4-thiadiazoles are presented here as new molecules able to decrease neuronal cell death and to increase endogenous neurogenesis blocking the GSK-3 substrate site

Synthesis and Biological Evaluation of 2,3,5-Substituted [1,2,4]Thiadiazoles as Allosteric Modulators of Adenosine Receptors

A number of 2,3,5-substituted [1,2,4]thiadiazole analogues of SCH-202676 (N-(2,3-diphenyl-[1,2,4]thiadiazole-5(2H)-ylidene)methanamine, 7a) were synthesized and tested as potential allosteric modulators of adenosine receptors. All compounds were capable of displacing the binding of the radiolabeled agonist [3H]CCPA to human A1 adenosine receptors, whereas modest and varying effects were observed on the binding of [3H]DPCPX, a radiolabeled antagonist for this receptor subtype. Four compounds, 7a (SCH-202676), 7k (LUF5792), 71 (LUF5794), and 8e (LUF5789), were selected for more detailed characterization. They all proved allosteric inhibitors of agonist binding, with 7k being most potent, whereas their effects on antagonist binding were more ambiguous. Subsequently, experiments were done on human adenosine A2A and A3 receptors. Compounds 7a and 7l displayed peculiar displacement characteristics of both radiolabeled agonist and antagonist binding to A2A receptors, whereas 7a showed some activity on A3 receptors.