200347-57-5Relevant academic research and scientific papers
Structural Simplification of Marine Natural Products: Discovery of Hamacanthin Derivatives Containing Indole and Piperazinone as Novel Antiviral and Anti-phytopathogenic-fungus Agents
Chen, Jianxin,Duan, Zhongyu,Li, Hongyan,Li, Lin,Lu, Aidang,Wang, Qingmin,Wang, Tienan,Zhou, Yanan
, p. 10093 - 10103 (2021)
With the increasing severity of plant diseases and the emergence of pathogen resistance, there is an urgent need for the development of new efficient and environment-friendly pesticides. Marine natural product (MNP) resources are rich and diverse. Structural simplification based on MNPs is an important strategy to find novel pesticide candidates. In this work, the marine natural product 6″-debromohamacanthin A (1a) was efficiently prepared and selected as the parent structure. A series of hamacanthin derivatives were designed, synthesized, and studied on the antiviral and antifungal activities. Most of these compounds displayed higher antiviral activities than ribavirin. The antiviral activities of compounds1aand13e-13hare similar to or higher than that of ningnanmycin (perhaps the most efficient anti-plant-virus agent). Compound13hwas selected for further antiviral mechanism research via transmission electron microscopy, molecular docking, and fluorescence titration. The results showed that compound13hcould bind to TMV CP and interfere with the assembly process of TMV CP and RNA. In addition, these hamacanthin derivatives also exhibited broad-spectrum inhibitory effects against eight common agricultural pathogens. Compounds1a12b, and12fwith excellent fungicidal activities can be considered as new fungicidal candidates for further research. These results provide a basis for the application of hamacanthin alkaloids in crop protection.
NOVEL BIS-INDOLIC DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS A DRUG
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Paragraph 0194; 0195, (2013/03/26)
The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
BIS-INDOLIC DERIVATIVES, THEIR USES IN PARTICULAR AS ANTIBACTERIALS
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Page/Page column 25; 26, (2013/03/26)
The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
BIS-INDOLIC DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS A DRUG
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Page/Page column 34; 35; 36, (2013/03/26)
The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
Synthesis and evaluation of 1-(1H-indol-3-yl)ethanamine derivatives as new antibacterial agents
Burchak, Olga N.,Pihive, Emmanuelle Le,Maigre, Laure,Guinchard, Xavier,Bouhours, Pascale,Jolivalt, Claude,Schneider, Dominique,Maurin, Max,Giglione, Carmela,Meinnel, Thierry,Paris, Jean-Marc,Denis, Jean-No?l
experimental part, p. 3204 - 3215 (2011/06/25)
A collection of 3-substituted indole derivatives was prepared using nucleophilic addition of indoles to nitrones. The compounds were then tested for their antibacterial activity against almost thirty bacterial strains representative of common human pathog
NOVEL INDOLIC DERIVATIVES, THEIR PREPARATION PROCESSES AND THEIR USES IN PARTICULAR AS ANTIBACTERIALS
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Page/Page column 33, (2010/06/19)
The invention relates to the use of at least one compound of the formula (I), in which R and R3 are particularly a hydrogen atom, R1 is particularly a hydrogen atom or a methyl, ethyl or isobutyl mi group, R4, R5, R6 and R7 are independently a hydrogen atony, an alkoxyl group with 1 to 7 carbon atoms or a halogen atom, R2 is a hydrogen atom, an O? group or an OH group, B is an N-GP1 or NRc, group, GP1 being a Boc or Cbz group, and Rc is a hydrogen atom or a methyl or t-butyl group, for preparing a drug for treating conditions associated with bacterial infections, in particular for treating bacterial diseases.
The reactions of nitrones with indoles
Chalaye-Mauger, Hélène,Denis, Jean-No?l,Averbuch-Pouchot, Marie-Thérèse,Vallée, Yannick
, p. 791 - 804 (2007/10/03)
The reaction of nitrones with various indole derivatives has been studied. When the reaction was promoted by C1SiMe3, the isolated products were 3,3'-diindolylalkanes. With HC1 as the activating reagent, 3- indolylhydroxylamines were isolated. The diastereoselectivity of this condensation with a nitrone derived from cysteine was investigated. A method for the introduction of an alkylhydroxylamino group onto position 2 of indole, the synthesis of three natural 3,3'-diindolylalkanes and of non- symmetric diindolylalkanes are also reported. (C) 2000 Elsevier Science Ltd.
The reaction of nitrones with indoles. Synthesis of asymmetrical diindolylalcanes
Denis, Jean-Noel,Mauger, Helene,Vallee, Yannick
, p. 8515 - 8518 (2007/10/03)
The reaction of nitrones with indoles in the presence of HCl gives indolyl N-hydroxylamines. In the presence of Me3SiCl symmetrical diindolylalcanes are obtained. A synthesis of asymmetrical diindolylalcanes and the syntheses of three natural symmetrical diindolylalcanes are reported.
