113501-99-8

Upstream product

• 71-23-8 propan-1-ol 
• 2369-11-1 5-fluoro-2-nitroaniline 
• 394-41-2 3-fluoro-4-nitrophenol 
• 28987-49-7 2-fluoro-1-nitro-4-propoxybenzene 
• 70599-87-0 (3-nitro-phenyl)-propyl ether 
• 4469-79-8 3-propoxyaniline 
• 554-84-7 meta-nitrophenol 
• 55792-52-4 acetic acid-(3-propoxy-anilide) 
• 130349-21-2 acetic acid-(2-nitro-5-propoxy-anilide) 
• 84437-62-7 4-Propyloxy-2-chlor-nitrobenzol 

Downstream Products

• 342043-33-8 N-acetyl-sulfanilic acid-(2-nitro-5-propoxy-anilide) 
• 1446282-02-5 2-chloro-N-(2-nitro-5-propoxyphenyl)acetamide 
• 1446282-03-6 N-(2-nitro-5-propoxyphenyl)-2-piperidylacetamide 
• 1446282-04-7 N-(2-amino-5-propoxyphenyl)-2-piperidylacetamide 
• 1446282-05-8 N-(2-{[2-(2,6-dimethylphenoxy)ethyl]amino}-5-propoxyphenyl)-2-piperidylacetamide 
• 1446281-89-5 1-[2-(2,6-dimethylphenoxy)ethyl]-2-piperidin-1-ylmethyl-5-propoxy-1H-benzimidazole 
• 56190-17-1 4-n-propoxy-o-phenylenediamine 

Relevant academic research and scientific papers

2-substituted thioacetamide compound, and preparation method and application thereof

The invention discloses a 2-substituted thioacetamide compound, and a preparation method and an application thereof. The structure of the 2-substituted thioacetamide compound is represented by formulaI, and R in the formula I is a C1-C3 alkoxy group, halogen or NR1R2, wherein R1 and R2 are H and a C1-C3 alkyl group independently. The compound can effectively inhibit protein-arginine methyltransferase 5, and can be used as a PRMT5 inhibitor.

Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization

PRMT5 plays important roles in diverse cellular processes and is upregulated in several human malignancies. Besides, PRMT5 has been validated as an anticancer target in mantle cell lymphoma. In this study, we found a potent and selective PRMT5 inhibitor by performing structure-based virtual screening and hit optimization. The identified compound 17 (IC50 = 0.33 μM) exhibited a broad selectivity against a panel of other methyltransferases. The direct binding of 17 to PRMT5 was validated by surface plasmon resonance experiments, with a Kd of 0.987 μM. Kinetic experiments indicated that 17 was a SAM competitive inhibitor other than the substrate. In addition, 17 showed selective antiproliferative effects against MV4-11 cells, and further studies indicated that the mechanism of cellular antitumor activity was due to the inhibition of PRMT5 mediated SmD3 methylation. 17 may represent a promising lead compound to understand more about PRMT5 and potentially assist the development of treatments for leukemia indications.

BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT

The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said compound, wherein variables R, R1, R2, R3, R4, R5, m, and n in Formula I are as defined herein