- COMPOSITIONS AND METHODS COMPRISING SUBSTITUTED 2-AMINOIMIDAZOLES
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The present invention presents 2-(acylamino)imidazoles with therapeutic activity, including selective activity against cancer cells, and compositions comprising them. Methods of using and preparing the 2-(acylamino)imidazoles are also presented.
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Paragraph 0189; 0190
(2018/10/25)
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- Polycarpine derivatives, synthesis of derivatives and application of derivatives in control of plant viruses and pathogenic bacteria
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The invention relates to Polycarpine derivatives, preparation of the derivatives and an application of the derivatives in controlling plant viruses and pathogenic bacteria. A meaning of R in the formula is as shown in the description. The Polycarpine deri
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Paragraph 0038; 0039; 0040; 0041;
(2018/01/04)
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- First discovery of polycarpine, polycarpaurines A and C, and their derivatives as novel antiviral and antiphytopathogenic fungus agents
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Marine natural products polycarpine, polycarpaurines A and C, and their derivatives were designed, synthesized, and characterized on the basis of 1H NMR and mass spectroscopy. The antiviral and antiphytopathogenic fungus activities of these alkaloids were first evaluated. Polycarpine derivative 1g displayed excellent in vivo antiviral activity against TMV (inactivation inhibitory effect, 57%/500 μg mL-1 and 19%/100 μg mL-1; curative inhibitory effect, 62%/500 μg mL-1 and 23%/100 μg mL-1; and protection inhibitory effect, 56%/500 μg mL-1 and 29%/100 μg mL-1), which is evidently higher than the activity of ribavirin (inactivation inhibitory effect, 37%/500 μg mL-1 and 9%/100 μg mL-1; curative inhibitory effect, 36%/500 μg mL-1 and 13%/100 μg mL-1; and protection inhibitory effect, 39%/500 μg mL-1 and 17%/100 μg mL-1), thus emerging as a new lead compound for antiviral research against TMV. Fungicidal testing in vitro showed that most of the compounds displayed good fungicidal activity against plant pathogenic fungi. Further in vivo fungicidal testing indicated that compounds 6a, 6f, and 8a-c displayed good fungicidal activity. Current results provide support for the development of polycarpine alkaloids as novel agrochemicals.
- Guo, Pengbin,Wang, Ziwen,Li, Gang,Liu, Yuxiu,Xie, Yunfu,Wang, Qingmin
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p. 4264 - 4272
(2016/06/15)
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- PROCESS FOR PREPARING N-METHYL-3, 4-DIMETHOXYPHENYLETHYLAMINE
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Provided are intermediates useful for the preparation of verapamil and methods for their preparation.
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Page/Page column 7
(2009/07/17)
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- Synthesis of polycarpine, a cytotoxic sulfur-containing alkaloid from the ascidian Polycarpa Aurata, and related compounds
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Polycarpine 1, a highly cytotoxic marine natural product, has been synthesized in three steps from p-methoxyphenacyl bromide 4 in 57% overall yield. The key reaction for construction of the symmetrically substituted disulfide linkage of polycarpine is the treatment of 2-amino-4-(4-methoxyphenyl)-1-methylimidazole 17 with S2Cl2 in acetic acid. In a similar way ten related compounds, including three thiazole analogues, have been prepared. Most of them exhibit high cytotoxic activities against an array of human cancer cell lines.
- Radchenko, Oleg S.,Novikov, Vyacheslav L.,Willis, Richard H.,Murphy, Peter T.,Elyakov, George B.
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p. 3581 - 3584
(2007/10/03)
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