3153-96-6

Upstream product

• 32263-14-2 4-hydroxy-3-methoxy-5-methylbenzaldehyde 
• 28276-04-2 3-(chloromethyl)-4-hydroxy-5-methoxybenzaldehyde 
• 87743-10-0 3-((dimethylamino)methyl)-4-hydroxy-5-methoxybenzaldehyde 
• 121-33-5 vanillin 
• 488-17-5 3-methylbenzene-1,2-diol 
• 80547-77-9 3-methyl-4,5-dimethoxybenzoic acid 
• 80547-86-0 3-methyl-4,5-dihydroxyacetophenone 
• 35236-40-9 3-methylpyrocatechol diacetate 
• 75-52-5 nitromethane 
• 80547-80-4 3,4-dimethoxy-5-methylbenzaldehyde 

Downstream Products

• 80547-83-7 2-nitro-3-methyl-4,5-dimethoxy-β-nitrostyrene 

Relevant academic research and scientific papers

Tetrahydrocoptisine derivative and applications thereof

The present invention relates to a compound as shown in a formula (VII), a preparation method and applications thereof in medicines. In particular, the present invention relates to a derivative of the compound as shown in the formula (VII), a preparation method, and the applications of the derivative used as a therapeutic agent in prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, II-type diabetes, hyperglycemia, obesity or insulin resistance syndrome and metabolic syndrome. The compound disclosed by the present invention can also reduce total cholesterol, LDL-cholesterol and triglyceride, and increases expression of a liver LDL receptor and decreases expression of PCSK9.

Catechol O-methyltransferase. 12. Affinity Labeling the Active Site with the Oxidation Products of 5,6-Dihydroxyindole

5,6-Dihydroxyindole (5,6-DHI) and a series of 4- and/or 7-methylated analogues of 5,6-DHI have been synthesized and evaluated for their ability to inactivate purified liver rat catechol O-methyltransferase (COMT).The inactivation of COMT by these agents could be prevented by excluding oxygen from the incubation mixtures, indicating the necessity for their oxidation to the corresponding aminochromes.Substrate protection studies and kinetic studies suggested that the loss of enzyme activity resulted from the modification of a crucial amino acid residue at the active site of COMT through reaction with the quinoid oxidation products.The COMT inhibitory activity of the 4- and/or 7-methylazed analogues of 5,6-DHI argue against a mechanism involving a 1,4 Michael addition reaction at positions 4 or 7 on the aminochrome.Cnsidering the number of potential eletrophilic centers on the basic aminochrome structure, the site of the reaction might change depending on the aromatic substitution pattern.The preferred pathway of reaction may be determined in part by the juxtaposition of the protein nucleophile to the possible sites of attack on the electrophilic ligand but also in part on the reactivity of the electrophilic site which might change with substitution on the aromatic ring.