82613-08-9

Upstream product

• 17892-42-1 O,O-diethylmelannein 
• 2651-55-0 3-ethoxy-4-methoxybenzoic acid 

Downstream Products

• 1349175-47-8 N-(3,5-dichloropyridin-4-yl)-3-ethoxy-4-methoxybenzamide 
• 82613-11-4 6-Hydroxy-7-methoxy-4-(3'-ethoxy-4'-methoxyphenyl)coumarin 
• 82613-10-3 Ethyl m-ethoxy-p-methoxybenzoylacetate 
• 31526-71-3 3-ethoxy-4-methoxy-acetophenone 
• 17892-42-1 O,O-diethylmelannein 
• 1092789-44-0 2-((3-ethoxy-4-methoxyphenyl)carbonyl)malononitrile 
• 17892-45-4 3'.5-Diethoxy-2.4.4'-trimethoxy-benzophenon 
• 17892-44-3 2-Hydroxy-3'.5-diethoxy-4.4'-dimethoxy-benzophenon 
• 17892-47-6 3'.4-Diethoxy-2.5.4'-trimethoxy-benzophenon 
• 18008-38-3 2-Hydroxy-3'.4-diethoxy-4'.5-dimethoxy-benzophenon 
• 203395-36-2 3-ethoxy-4,3',4'-trimethoxy-benzophenone 

Relevant academic research and scientific papers

Ambroxol derivative, and preparation method, medicinal composition and application thereof

The invention relates to the field of medicinal chemistry, and concretely relates to an ambroxol derivative or pharmaceutically acceptable salts thereof, and a preparation method, a medicinal composition and a medical application thereof. The ambroxol derivative is a compound with a structure represented by formula I shown in the specification, and R in the formula I is defined in claims.

Pharmacological validation of trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness

Neglected tropical disease drug discovery requires application of pragmatic and efficient methods for development of new therapeutic agents. In this report, we describe our target repurposing efforts for the essential phosphodiesterase (PDE) enzymes TbrPDEB1 and TbrPDEB2 of Trypanosoma brucei, the causative agent for human African trypanosomiasis (HAT). We describe protein expression and purification, assay development, and benchmark screening of a collection of 20 established human PDE inhibitors. We disclose that the human PDE4 inhibitor piclamilast, and some of its analogues, show modest inhibition of TbrPDEB1 and B2 and quickly kill the bloodstream form of the subspecies T. brucei brucei. We also report the development of a homology model of TbrPDEB1 that is useful for understanding the compound-enzyme interactions and for comparing the parasitic and human enzymes. Our profiling and early medicinal chemistry results strongly suggest that human PDE4 chemotypes represent a better starting point for optimization of TbrPDEB inhibitors than those that target any other human PDEs.

Kinase antagonists

The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tryosine kinase, PI3Kinase and mTOR, or PI3Kinase, mTOR and tryosine kinase.

An Unambiguous Synthesis of Melannein

Melannein (6-hydroxy-7-methoxy-4-(3'-hydroxy-4'-methoxyphenyl)coumarin, I) and its O,O-diethyl ether (II) have been synthesised.The steps involved in the synthesis of I and II are the respective condensation of o-methoxyhydroquinone with ethyl m-benzyloxy-p-methoxybenzoylacetate (XI) and ethyl m-ethoxy-p-methoxybenzoylacetate (III) in absolute ethyl alcohol in the presence of dry hydrogen chloride gas.The isomeric O,O-diethyl ether of melannein, viz. 6-ethoxy-7-methoxy-4(4'-ethoxy-3'-methoxyphenyl)coumarin (VI) has also been prepared by the condensation of o-methoxyhydroquinone with ethyl p-ethoxy-m-methoxybenzoylacetate (VII).The esters (III), (VII) and (XI) have been prepared by the reaction of the appropriate acetophenone derivatives with diethyl carbonate in the presence of sodium hydride.