84427-30-5

Upstream product

• 1747-60-0 6-methoxybenzothiazol-2-ylamine 
• 1885-14-9 phenyl chloroformate 
• 2293-07-4 1-(4-methoxyphenyl)thiourea 

Downstream Products

• 866001-38-9 4-(3-(6-methoxybenzo[d]thiazol-2-yl)ureido)benzoic acid 

Relevant academic research and scientific papers

Discovery of Hydroxybenzothiazole Urea Compounds as Multitargeted Agents Suppressing Major Cytotoxic Mechanisms in Neurodegenerative Diseases

Multiple factors are causally responsible and/or contribute to the progression of Alzheimer's and Parkinson's diseases. The protein kinase Dyrk1A was identified as a promising target as it phosphorylates tau protein, α-synuclein, and parkin. The first goal of our study was to optimize our previously identified Dyrk1A inhibitors of the 6-hydroxy benzothiazole urea chemotype in terms of potency and selectivity. Our efforts led to the development of the 3-fluorobenzyl amide derivative 16b, which displayed the highest potency against Dyrk1A (IC50 = 9.4 nM). In general, the diversification of the benzylamide moiety led to an enhanced selectivity over the most homologous isoform, Dyrk1B, which was a meaningful indicator, as the high selectivity could be confirmed in an extended selectivity profiling of 3b and 16b. Eventually, we identified the novel phenethyl amide derivative 24b as a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers. We provide evidence that the novel combination of selective Dyrk1A inhibition and suppression of tau and α-syn aggregations of our new lead compound confers efficacy in several established cellular models of neurotoxic mechanisms relevant to neurodegenerative diseases, including α-syn-and 6-hydroxydopamine-induced cytotoxicities.

Design and synthesis of conformationally constraint Dyrk1A inhibitors by creating an intramolecular H-bond involving a benzothiazole core

We present the development of conformationally pre-organised Dyrk1A inhibitors based on the hydroxybenzothiazole urea scaffold. The modifications introduced to the discovered hit (AHS-211) proved the crucial role of the urea linker to preserve the bioacti

Synthesis of substituted benzo[d]thiazol-2-ylcarbamates as potential anticonvulsants

A series of substituted benzo[d]thiazol-2-ylcarbamates 4a-g and 5a-g were synthesized and evaluated for anticonvulsant activity. The structures of the synthesized compounds were confirmed on the basis of their physical and spectral data. The compounds were evaluated for anticonvulsant activity using PTZ-induced convulsion and maximal electroshock models. The target compounds have shown significant activity in these models.