6938-68-7Relevant articles and documents
Antiviral compound and preparation method thereof
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Paragraph 0075-0078, (2021/04/28)
The invention discloses an antiviral compound and a preparation method thereof. The structural formula of the compound is shown as a formula I in the specification. In the formula (I), R is selected from mono-substituted or multi-substituted H, F, a methyl group and a trifluoromethyl group; R is selected from H, a linear or substituted alkane (C1C6); R is selected from monosubstituted or polysubstituted H, Cl, Br and F; when X is NH, R is selected from H and an acyl group including a sulfonyl group, a phosphoryl group or an alkanoyl group; and when X is O, R is as described in the specification, n is an integer in a range of 0 to 6, such as 2 or 3, and Y is selected from O and N. Experiments prove that the compound provided by the invention not only has a good inhibition effect on H1N1 influenza A virus, but also has a good inhibition effect on coronavirus; the toxicity of the compound to human normal cells does is not found during observation; and the compound can inhibit the degree of inflammatory response while resisting viruses.
A 2-methyl amino thiourea synthesis method
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Paragraph 0024; 0025, (2017/01/17)
The invention relates to a synthetic method for 2-methylthiosemicarbazide, which belongs to the field of chemical synthesis. The method comprises the following steps: adding 40% of an aqueous methylhydrazine solution, ammonium thiocyanate and an inorganic salt catalyst according to a certain mass ratio into an enameled reaction vessel with a volume of 5000 L; carrying out a dehydration reaction at a temperature of 112 to 115 DEG C for 4 to 5 h; introducing circulating water for cooling to room temperature after completion of the reaction; carrying out centrifugal filtration by using a centrifuge; and taking a precipitate at a lower layer and drying the precipitate with a double-cone rotary vacuum dryer for 2 to 4 h so as to obtain 2-methylthiosemicarbazide. The method provided by the invention has simple reaction steps and enables yield to be greatly improved through usage of an inorganic ferric salt catalyst, the yield of 2-methylthiosemicarbazide reaches 95.8 to 96.8%, and production cost is reduced by more than 30% compared with a traditional process.
Structure-based design of potent human dihydroorotate dehydrogenase inhibitors as anticancer agents
Song, Wenlin,Li, Shiliang,Tong, Yi,Wang, Jiawei,Quan, Lina,Chen, Zhuo,Zhao, Zhenjiang,Xu, Yufang,Zhu, Lili,Qian, Xuhong,Li, Honglin
supporting information, p. 1441 - 1448 (2016/07/21)
It has been proven that inhibiting human dihydroorotate dehydrogenase (hDHODH) restricts the growth of rapidly proliferating cells, thus hDHODH can be developed as a promising target for the treatment of immunological disease and cancer. Here, a succession of substituted hydrazino-thiazole derivatives were designed, synthesized, and biologically evaluated through structure-based optimization, of which compound 22 was the most potent inhibitor of hDHODH with an IC50 value of 1.8 nM. Furthermore, 22 exhibited much better antiproliferative activity than brequinar, both in HCT-116 and BxPC-3 cancer cell lines. Flow cytometry analysis revealed that 22 induced S phase cell cycle arrest and promoted induction of apoptosis. All results established a proof that blocking the pyrimidine de novo synthesis pathway by inhibiting the rate-limiting enzyme hDHODH is an attractive therapy for cancer.
