38588-55-5

Upstream product

• 486-66-8 daidzein 
• 105-36-2 ethyl bromoacetate 
• 68747-24-0 ethyl 2-(3-hydroxyphenoxy)acetate 
• 14191-95-8 4-cyanomethylphenol 
• 122-51-0 orthoformic acid triethyl ester 

Relevant academic research and scientific papers

Structural modification and antihypertensive activity study of formononetin derivatives

A series of formononetin derivatives with substituted benzyloxy groups on the 4′ position of isoflavone were designed and synthesized. Their vasodilative activities were evaluated by wire myograph system on isolated rat mesenteric arterial ring. The preli

Daidzein semiantigen and complete antigen and preparation method and application

The invention discloses daidzein semiantigen and complete antigen and a preparation method and an application thereof. Molecular structure of the daidzein semiantigen is as shown in the formula (I) or the formula (II). Daidzein used as a raw material undergoes two steps of chemical reactions to respectively obtain daidzein 7-derivative and 4'-derivative semiantigen, and daidzein semiantigen is successively synthesized. The synthetic method is safe and effective, and purity of the products is high. On this basis, daidzein complete antigen suitable for animal immunization is further prepared by an active ester method. By using the antigen to immunize Balb/c mouse, titer can reach 1:32000, and inhibition rate can reach 94.9%. Core raw materials and favorable conditions are provided for establishment of a daidzein immunization analysis method. The product has a wide practical application prospect.

COMPOUNDS USEFUL FOR THE INHIBITION OF ALDH

The present invention provides novel antidipsotropic compounds. The invention further provides methods of inhibiting ALDH-2 using the compounds described herein. Methods for modulating alcohol consumption, alcohol dependence and/or alcohol abuse by administering the compounds of the invention to an individual are also provided. The present invention further provides a rationale for designing additional novel antidipsotropic compounds.

Synthesis of potential antidipsotropic isoflavones: Inhibitors of the mitochondrial monoamine oxidase - Aldehyde dehydrogenase pathway

Recently we have shown that daidzin, the major active principle of an ancient herbal treatment for quot;alcohol addictionquot; suppresses ethanol intake in alcohol-preferring laboratory animals. Further, we have identified the monoamine oxidase (MAO) - aldehyde dehydrogenase (ALDH-2) pathway of the mitochondria as the potential site of action of daidzin. Daidzin analogues that potently inhibit ALDH-2 but have no or little effect on MAO are most antidipsotropic, whereas those that also inhibit MAO exhibit little, if any, antidipsotropic activity. Therefore, in the design and synthesis of more potent antidipsotropic analogues, structural features important for the inhibition of both ALDH-2 and MAO must be taken into consideration. To gain further information on the structure-activity relationships at the inhibitor binding sites of ALDH-2 and MAO, we prepared 44 analogues of daidzin and determined their potencies for ALDH-2 and MAO inhibition. Results indicate that a sufficient set of criteria for a potent antidipsotropic analogue is an isoflavone with a free 4′-OH function and a straight-chain alkyl substituent at the 7 position that has a terminal polar function such as -OH, -COOH, or -NH2. The preferable chain lengths for the 7-O-ω-hydroxy, 7-O-ω-carboxy, and 7-O-ω-amino subsitutents are 2 ≤ n ≤ 6, 5 ≤ n ≤ 10, and n ≥ 4, respectively. Analogues that meet these criteria have increased potency for ALDH-2 inhibition and/or decreased potency for MAO inhibition and therefore are likely to be potent antidipsotropic agents.

Ground mixture

A ground mixture of a poorly soluble crystalline drug and an adsorbent is remarkably improved in the rates of dissolution and adsorption of the drug.