17746-77-9

Upstream product

• 22717-57-3 methyl 6-hydroxy-m-toluate 
• 186581-53-3 diazomethane 
• 17746-75-7 3-bromo-5-methylsalicylic acid 

Downstream Products

• 43135-49-5 2-bromo-6-(hydroxymethyl)-4-methyl-phenol 
• 1228005-48-8 (E)-1-(3-bromo-2-hydroxy-5-methylphenyl)-3-(2-chloro-6-ethoxyquinolin-3-yl)prop-2-en-1-one 

Relevant academic research and scientific papers

WDR5 INHIBITORS AND MODULATORS

Described are imino-azacycle-benzamide compounds compounds that inhibit WDR5 and associated protein-protein interactions, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and c

Studies on enzyme-cleavable dialkoxymethyl-cycloSaligenyl-2′, 3′-dideoxy-2′,3′-didehydrothymidine monophosphates

Recently we reported on conceptually new enzymatically activated cycloSal-pronucleotides. Now, we developed this concept further with new compounds of this type. The basic idea is fast intracellular cleavage of a functionalized group at the cycloSal residue that results in a rapid delivery of the nucleotide and thus an intracellular enrichment of the nucleotide. The introduction of a higher alkylated acylal group, the di-iso-butyryloxymethyl group, to the aromatic ring led to the expected higher stability of these prodrugs against enzymatic cleavage but also entailed surprisingly a decrease in hydrolysis stabilities and solubility problems. For some compounds, a separation of the two diastereomeric forms (RP or SP) was achieved. By X-ray structure analysis, the absolute configuration at the P-atom was assigned. For all separated diastereomers the (SP) form showed better antiviral activity than the (RP) form.

Derivatives of 1,4-bis(3-hydroxycarbonyl-4-hydroxyl)styrylbenzene as PTP1B inhibitors with hypoglycemic activity

Disalicylic acid derivatives with stilbene and bis-styrylbenzene skeleton were synthesized as PTP1B inhibitors. The most potent in this series exhibited a submicromolar IC50 value. One of the compounds 7b was tested in an animal model for its efficacy as an anti-diabetic or an anti-obesity agent. In feeding compound 7b to diet-induced obese mice, no significant differences in weight gain and food consumption were observed between the drug-treated and the obese control mice. However, 7b significantly lowered the fasting glucose level and improved the glucose tolerance in the obesity-induced diabetic mice.