329921-62-2

Upstream product

• 79-19-6 thiosemicarbazide 
• 1878-68-8 2-(4-bromophenyl)-acetic acid 

Downstream Products

• 1310578-64-3 2-(4-bromobenzyl)-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazole 

Relevant academic research and scientific papers

Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study

Sirtuins are NAD+-dependent protein deacylases that cleave off acetyl but also other acyl groups from the ε-amino group of lysines in histones and other substrate proteins. Dysregulation of human Sirt2 (hSirt2) activity has been associated with the pathogenesis of cancer, inflammation, and neurodegeneration, which makes the modulation of hSirt2 activity a promising strategy for pharmaceutical intervention. The sirtuin rearranging ligands (SirReals) have recently been discovered by us as highly potent and isotype-selective hSirt2 inhibitors. Here, we present a well-defined structure-activity relationship study, which rationalizes the unique features of the SirReals and probes the limits of modifications on this scaffold regarding inhibitor potency. Moreover, we present a crystal structure of hSirt2 in complex with an optimized SirReal derivative that exhibits an improved in vitro activity. Lastly, we show cellular hyperacetylation of the hSirt2 targeted tubulin caused by our improved lead structure.

Synthesis and evaluation of 5-benzyl-1,3,4-thiadiazole derivatives as acetylcholinesterase inhibitors

Three novel 5-benzyl-1,3,4-thiadiazole derivatives were synthesised starting from phenylacetic acid derivatives. These compounds were characterised by NMR, HRMS and single-crystal X-ray diffraction analysis. 2-Pyrrolidyl-5-[2-(4-bromophenyl)methyl]-1,3,4-

Synthesis, characterisation and acetylcholinesterase-inhibition activities of 5-benzyl-1,3,4-thiadiazol-2-amine derivatives

Four 5-benzyl-1,3,4-thiadiazol-2-amine derivatives were synthesised from phenylacetic acid derivatives. The structures of the 5-benzyl- 1,3,4-thiadiazole derivatives were characterised by NMR spectroscopy and X-ray crystallography. The acetylcholinesteras

Preparation of 2-amino-5-alkyl -1, 3, 4-thiadiazole

The invention discloses a method for preparing 2-amino-5-alkyl-1,3,4-thiadiazole. The method comprises the following steps of adding A mol of thiosemicarbazide, B mol of carboxylic acid, C mol of phosphorus oxychloride and D mol of silica gel in a dry reaction container, grinding at a room temperature until the raw materials are completely reacted, and standing to obtain a crude product, wherein A: B: C = 1: (1 to 1.2): (1 to 1.2), and A: D = 1: (5 to 10); then adding alkaline solution in the crude product until the pH value of the obtained mixed solution is 8-8.2, then carrying out suction filtration on the mixed solution, dissolving the filter cake by a solvent and then further carrying out suction filtration, removing silica gel, then carrying out reduced pressure concentration on the finally-obtained filtrate, and removing the solvent to obtain 2-amino-5-alkyl-1,3,4-thiadiazole. The method disclosed by the invention is a solid-phase reaction, silica gel is used as a carrier, the operation process is simple, the reaction time is short, the reaction conditions are moderate, the equipment requirements are low, and the yield of the target product is up to more than 91%.

Synthesis and biological evaluation of novel 2-aralkyl-5-substituted-6- (4′-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent anticancer agents

Levamisole, the imidazo[2,1-b]thiazole derivative has been reported as a potential antitumor agent. In the present study, we synthesized, characterized and evaluated biological activity of its novel analogues with substitution in the aralkyl group and on