7150-04-1Relevant academic research and scientific papers
Preparation methods of three kinds of methyl uric acid compounds, intermediate and preparation method of the intermediate
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Paragraph 0163; 0164; 0165, (2019/01/07)
The invention provides preparation methods of three types of compounds which can be extracted from plants such as tea trees and have the effects of resisting depression, tranquilizing and hypnosis, resisting inflammation and easing pain, reducing stress damage of the liver cells and improving the exercise ability, an intermediate and a preparation method of the intermediate. The method is simple and convenient to operate, high in safety, high in atom economy and less in three wastes, and the raw and auxiliary materials are cheap and easy to obtain, low in toxicity, safe and stable; the reaction conditions are mild, the impurities are few, and the yield is high. The product is purified by crystallization, column chromatography is avoided, the operation is simple and feasible, and the process is stable, easy to control and convenient in reaction after-treatment, and can be economically and conveniently used for industrial production.
Fragment Discovery for the Design of Nitrogen Heterocycles as Mycobacterium tuberculosis Dihydrofolate Reductase Inhibitors
Shelke, Rupesh U.,Degani, Mariam S.,Raju, Archana,Ray, Mukti Kanta,Rajan, Mysore G. R.
, p. 602 - 613 (2016/08/28)
Fragment-based drug design was used to identify Mycobacterium tuberculosis (Mtb) dihydrofolate reductase (DHFR) inhibitors. Screening of ligands against the Mtb DHFR enzyme resulted in the identification of multiple fragment hits with IC50 values in the range of 38–90 μM versus Mtb DHFR and minimum inhibitory concentration (MIC) values in the range of 31.5–125 μg/mL. These fragment scaffolds would be useful for anti-tubercular drug design.
Synthesis and antitumor activity of new pyrimidine and caffeine derivatives
Abu-Hashem, Ameen Ali,Hussein, Hoda Abdel Raouf
, p. 471 - 478 (2015/06/22)
6-Amino-1, 3-dimethyl-1H-pyrimidine-2, 4-dione 2 was prepared by alkylation of 6-amino-1H-pyrimidine-2, 4-dione 1 with methyl iodide. Formylation of 2 with formic acid afforded N-(1, 3-dimethyl-dioxo-tetrahydropyrimidin-4-yl)-formamide 3. The nitration of 3 gave N-(1,3-dimethyl-5-nitro-dioxo-tetrahydropyrimidin-4-yl) formamide 4. Reduction of 4 by zinc dust in glacial acetic acid yielded dimethyl-dihydro-purine-2, 6-dione 5. Addition of bromine to 2 leads to the formation of 6-amino-5-bromo-dimethyl-pyrimidine-2, 4-dione 7, cycloaddition of 7 with formamide afford the same product (theophylline 5), alkylated of 5 with methyl iodide to give caffeine 6. Reaction of 7 with glycine gave 2-(6-amino-dimethyl-dioxo-tetrahydropyrimidin-5-ylamino) acetic acid 8, refluxing of 8 with acetic acid /methanol gave dimethyl-dihydropyrimidopyrazine-trione 9, alkylation of 9 with alkyliodide afforded tetra-alkyldihydropyrimidopyrazine-trione 10a and 10b. The Cytotoxicity screen of the synthesized compounds was evaluated and the result showed that 10a, 10b, 9, 8, 7 and 6 exhibited highly potential antitumor activity.
