406192-82-3Relevant academic research and scientific papers
INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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Paragraph 0772-0774, (2019/05/15)
The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
Antibacterial compound and its salt
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Paragraph 0031-0033; 0035-0036, (2017/10/06)
The invention provides a compound of a formula I or a pharmaceutically acceptable salt, a hydrate or a crystal form thereof. An acyl group is connected with the fourth, fifth or sixth-site carbon atom of indolyl. Researches find that the compound provided by the invention has certain antibacterial activity, and can be used as a potential antibacterial drug or daily chemical. Beyond all expectations, a compound 4c is extremely similar to compounds 4a and 4b in structure, but the antibacterial activity of the compound 4c is obviously better than that of the other two compounds; the antibacterial activity of the compound 4c against staphylococcus aureus is significantly better than the antibacterial activity of the compound 4c against escherichia coli, which illustrates that the compound 4c is more sensitive to the staphylococcus aureus; and if being used for antibiosis, the compound 4c can more easily inhibit particular species (such as staphylococcus aureus) in a targeted way, so that the unnecessary drug resistance caused by other bacteria is avoided.
A double-indole hydrazone compound and use thereof
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Paragraph 0036; 0041, (2017/10/06)
The invention provides a bisindole acylhydrazone compound shown as the formula I or salt, hydrate or crystals, accepted in the pharmacy, of the bisindole acylhydrazone compound. According to the bisindole acylhydrazone compound, R does not exist or is selected from alkylene of C1-5. The bisindole acylhydrazone compound has a certain antibacterial activity, and can serve as potential antibiotics or a daily chemical product. What is beyond the expectation is that compounds 4e-4h and compounds 4a-4c are quite similar in structure, the antibacterial activity of the compounds 4e-4h and the antibacterial activity of the compounds 4a-4c are obviously better than that of other compounds, particularly, the activity of the compound 4h is best and is remarkably better than that of compounds 4e-4g. The formula I is shown in the specification.
A double-indole hydrazone compound and its salt (by machine translation)
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Paragraph 0032-0036; 0039-0040, (2017/10/06)
The present invention provides a bis-indole compounds shown as formula I hydrazone compound or its pharmaceutically acceptable salt, hydrate or crystalline form. Wherein R is selected from none or C1 - 3 alkylene. This invention discovers, the present invention provides compound has antibacterial activity, can be used as a potential antibacterial drug or of daily use. It is not expected to, compound 4 d with a compound 4a - 4c structure is extremely similar, but its antibacterial activity is obviously superior to other compound; and, compound 4 d to Staphylococcus aureus bacteriostatic activity to be improved to the role of the Escherichia coli, note compound 4 d to Staphylococcus aureus more sensitive, if the use of the compound of antibacterial, in limited under the dosage, more easily targeted inhibit specific bacteria (such as jin pujun), to avoid other bacteria produce unnecessary drug resistance. (by machine translation)
A antibacterial synthetic method of the compound
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Paragraph 0035-0037; 0039-0040, (2017/10/06)
The invention provides a synthesis method of a bisindolyl acylhydrazone compound represented by a formula I shown in specifications, wherein acyl is connected with a carbon atom of a 4-, 5- or 6-bit of indolyl. The synthesis method provided by the invention has the advantages of high speed, high efficiency, low solvent consumption and relatively high target compound yield, thereby providing a necessary basis for further researching the compound represented by the formula I or related compounds. An intermediate provided by the invention is simple in structure and is easy to obtain, so that convenience is provided for the preparation of target compounds.
Identification of N-acylhydrazone derivatives as novel lactate dehydrogenase A inhibitors
Rupiani, Sebastiano,Buonfiglio, Rosa,Manerba, Marcella,Di Ianni, Lorenza,Vettraino, Marina,Giacomini, Elisa,Masetti, Matteo,Falchi, Federico,Di Stefano, Giuseppina,Roberti, Marinella,Recanatini, Maurizio
supporting information, p. 63 - 70 (2015/06/30)
Abstract Glycolysis is drastically increased in tumors and it is the main route to energy production with a minor use of oxidative phosphorylation. Among the key enzymes in the glycolytic process, LDH is emerging as one of the most interesting targets for the development of new inhibitors. In this context, in the present work, we carried out a virtual screening procedure followed by chemical modifications of the identified structures according to a "hit-to-lead" process. The effects of the new molecules were preliminary probed against purified human LDH-A. The compounds active at low micromolar level were additionally characterized for their activity on some cellular metabolic processes by using Raji human cell line. Within the series, 1 was considered the best candidate, and a more detailed characterization of its biological properties was performed. In Raji cells exposed to compound 1 we evidenced the occurrence of effects usually observed in cancer cells after LDH-A inhibition: reduced lactate production and NAD/NADH ratio, apoptosis. The flow cytometry analysis of treated cells also showed cell cycle changes compatible with effects exerted at the glycolytic level. Finally, in agreement with the data obtained with other inhibitors or by silencing LDH-A expression, compound 1 was found to increase Raji cells response to some commonly used chemotherapeutic agents. Taken together, all these finding are in support of the LDH-A inhibiting activity of compound 1.
Microwave-assisted synthesis and molecular recognition properties of novel indole acylhydrazone receptors
Ye, Ying,Suo, Yourui,Yang, Fang,Yang, Yongjing,Han, Lijuan
, p. 296 - 299 (2015/06/02)
Indole acylhydrazones were synthesised in high yields under microwave irradiation By using indole carboxylic acid and 1,4-benzenedialdehyde as starting materials. Their structures were characterised by 1H NMR, IR, MS spectra and elemental analysis. Selective recognition properties of these receptors have been investigated by UV-Vis spectra titration indicating that these receptors can form 1:1 supramolecular complexes with malic acid, tartaric acid, ascorbic acid and tryptophan.
AZOLE COMPOUNDS AS PIM INHIBITORS
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Page/Page column 67, (2012/10/08)
The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further em
A facial synthesis and antimicrobial activity of some pyrazole derivatives carrying indole
Narasimha Sarma,Subha,Chow Doji Rao
experimental part, p. 745 - 750 (2012/01/06)
The title compounds (7a-h) were prepared by esterification of indole-5-carboxylic acid (1) and subsequent treatment with hydrazine hydrate in methanol via the hydrazide (3). Finally hydrazide (3) condensed with different substituted aldol (6) in acetic ac
INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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Page/Page column 121-122, (2010/11/04)
The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
