117292-19-0

Upstream product

• 4518-10-9 Methyl 3-aminobenzoate 
• 594-44-5 Ethanesulfonyl chloride 
• 849410-09-9 ethyl 3-[(ethylsulfonyl)amino]benzoate 
• 582-33-2 3-aminobenzoic acid ethyl ester 

Downstream Products

• 119085-54-0 Ethanesulfonic acid [2-acetyl-4-(3,4-dimethoxy-phenyl)-1,2,3,4-tetrahydro-isoquinolin-7-yl]-amide 
• 119085-51-7 N-[2-(3,4-Dimethoxy-phenyl)-2-hydroxy-ethyl]-3-ethanesulfonylamino-benzamide 
• 1026397-29-4 Ethanesulfonic acid [2-acetyl-4-(3,4-dihydroxy-phenyl)-1,2,3,4-tetrahydro-isoquinolin-7-yl]-amide 
• 119085-52-8 Ethanesulfonic acid (3-{[2-(3,4-dimethoxy-phenyl)-2-hydroxy-ethylamino]-methyl}-phenyl)-amide 
• 119085-53-9 Ethanesulfonic acid [4-(3,4-dimethoxy-phenyl)-1,2,3,4-tetrahydro-isoquinolin-7-yl]-amide 

Relevant academic research and scientific papers

Demonstrating Ligandability of the LC3A and LC3B Adapter Interface

Autophagy is the common name for a number of lysosome-based degradation pathways of cytosolic cargos. The key components of autophagy are members of Atg8 family proteins involved in almost all steps of the process, from autophagosome formation to their selective fusion with lysosomes. In this study, we show that the homologous members of the human Atg8 family proteins, LC3A and LC3B, are druggable by a small molecule inhibitor novobiocin. Structure-activity relationship (SAR) studies of the 4-hydroxy coumarin core scaffold were performed, supported by a crystal structure of the LC3A dihydronovobiocin complex. The study reports the first nonpeptide inhibitors for these protein interaction targets and will lay the foundation for the development of more potent chemical probes for the Atg8 protein family which may also find applications for the development of autophagy-mediated degraders (AUTACs).

NOVEL SULFONE AMIDE DERIVATIVES CAPABLE OF INHIBITING BACE

The present invention relates to novel derivatives of sulfone amide of Formula 1 as defined in this disclosure which inhibit the activity of BACE (or beta-secretase). These sulfone amide derivatives are useful for the treatment and prevention of Alzheimer's disease and related diseases caused by production of beta-amyloid, by inhibiting the activity of BACE.

4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline derivatives. II. Their renal vasodilation activity and structure-activity relationship

A series of 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline derivatives showed potent DA1 agonistic activities. We investigated the structure-activity relationship of the racemic compounds of this series. 4- (3,4-Dihydroxyphenyl)-7-metha