- A class of highly effective broad-spectrum plant antimicrobial agentS
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The present invention relates to a class of benzohydrazone compounds and synthetic methods thereof and drugs containing the compound thereof and applications thereof. The hydrate compounds involved in the present invention have the advantages of simple structure, easy synthesis, strong antibacterial activity, wide antibacterial spectrum, small toxicity to animals and plants and low composition, and can be used as active ingredients or synergistic ingredients for the development of new high-efficiency broad-spectrum plant antibacterial agents.
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Paragraph 0036; 0043-0045; 0065
(2022/03/27)
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- Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity
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Histone deacetylase 6 (HDAC6) has emerged as a critical regulator of many cellular pathways in tumors due to its unique structure basis and abundant substrate types. Over the past few decades, the role played by HDAC6 inhibitors as anticancer agents has sparked great interest of biochemists worldwide. However, they were less reported for gastric cancer therapy. In this paper, with the help of bioisosteric replacement, in-house library screening, and lead optimization strategies, we designed, synthesized and verified a series of 1,3-diaryl-1,2,4-triazole-capped HDAC6 inhibitors with promising anti-gastric cancer activities. Amongst, compound 9r displayed the best inhibitory activity towards HDAC6 (IC50 = 30.6 nM), with 128-fold selectivity over HDAC1. Further BLI and CETSA assay proved the high affinity of 9r to HDAC6. In addition, 9r could dose-dependently upregulate the levels of acetylated α-tubulin, without significant effect on acetylated histone H3 in MGC803 cells. Besides, 9r exhibited potent antiproliferative effect on MGC803 cells, and promoted apoptosis and suppressed the metastasis without obvious toxicity, suggesting 9r would serve as a potential lead compound for the development of novel therapeutic agents of gastric cancer.
- Zhang, Xin-Hui,Kang, Hui-Qin,Tao, Yuan-Yuan,Li, Yi-Han,Zhao, Jun-Ru,Ya-Gao,Ma, Li-Ying,Liu, Hong-Min
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- Iron-catalyzed aerobic oxidative cleavage of the C-C σ-bond using air as the oxidant: Chemoselective synthesis of carbon chain-shortened aldehydes, ketones and 1,2-dicarbonyl compounds
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A simple iron-catalyzed aerobic oxidative C-C σ-bond cleavage of ketones has been developed. Readily available and environmentally benign air is used as the oxidant. This reaction avoids the use of noble metal catalysts or specialized oxidants, chemoselectively yielding carbon chain-shortened aldehydes, ketones and 1,2-dicarbonyl compounds without overoxidation.
- Xing, Qi,Lv, Hui,Xia, Chungu,Li, Fuwei
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supporting information
p. 489 - 492
(2016/01/12)
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- Biological properties of heterocyclic pyridinylimines and pyridinylhydrazones
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This work describes the synthesis and biological properties of a series of 2- and 4- pyridinylimines and pyridinylhydrazones. All compounds were evaluated in vitro against two species of Leishmania. The antioxidant activity and the toxic effect against mu
- Martins, Francislene J.,Lima, Rebeca Mól,Dos Santos, Juliana Alves,De Almeida Machado, Patrícia,Coimbra, Elaine Soares,Da Silva, Adilson David,Raposo, Nádia Rezende Barbosa
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p. 107 - 114
(2015/11/17)
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- Biological properties of heterocyclic pyridinylimines and pyridinylhydrazones
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This work describes the synthesis and biological properties of a series of 2- and 4-pyridinylimines and pyridinylhydrazones. All compounds were evaluated in vitro against two species of Leishmania. The antioxidant activity and the toxic effect against mur
- Martins, Francislene J.,Lima, Rebeca Ml,Dos Santos, Juliana Alves,De Almeida Machado, Patricia,Coimbra, Elaine Soares,Da Silva, Adilson David,Raposo, Ndia Rezende Barbosa
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p. 107 - 114
(2015/12/01)
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- Potent antimicrobial agents against azole-resistant fungi based on pyridinohydrazide and hydrazomethylpyridine structural motifs
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Abstract Schiff base derivatives have recently been shown to possess antimicrobial activity, and these derivatives include a limited number of salicylaldehyde hydrazones. To further explore this structure-activity relationship between salicylaldehyde hydrazones and antifungal activity, we previously synthesized and analyzed a large series of salicylaldehyde and formylpyridinetrione hydrazones for their ability to inhibit fungal growth of both azole-susceptible and azole-resistant species of Candida. While many of these analogs showed excellent growth inhibition with low mammalian cell toxicity, their activity did not extend to azole-resistant species of Candida. To further dissect the structural features necessary to inhibit azole-resistant fungal species, we synthesized a new class of modified salicylaldehyde derivatives and subsequently identified a series of modified pyridine-based hydrazones that had potent fungicidal antifungal activity against multiple Candida spp. Here we would like to present our synthetic procedures as well as the results from fungal growth inhibition assays, mammalian cell toxicity assays, time-kill assays and synergy studies of these novel pyridine-based hydrazones on both azole-susceptible and azole-resistant fungal species.
- Backes, Gregory L.,Jursic, Branko S.,Neumann, Donna M.
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p. 3397 - 3407
(2015/08/03)
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- Nano BF3·SiO2: A green heterogeneous solid acid for synthesis of formazan dyes under solvent-free condition
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A solvent-free, efficient and rapid approach for synthesis of formazan dyes was developed by diazotization of aromatic amines with NaNO2, nano silica-supported boron trifluoride (nano BF3·SiO2), then diazo coupling with aldehyde phenylhydrazones by grinding method at room temperature. This study aimed to overcome the limitations and drawbacks of the previous reported methods such as: low temperature, using corrosive and toxic acids and solvents, using buffer solutions, instability of aryl diazonium salts, modest yields, and long reaction times.
- Bamoniri, Abdolhamid,Mirjalili, Bi Bi Fatemeh,Moshtael-Arani, Naimeh
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p. 272 - 278
(2014/07/22)
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- Fast hydrazone reactants: Electronic and acid/base effects strongly influence rate at biological pH
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Kinetics studies with structurally varied aldehydes and ketones in aqueous buffer at pH 7.4 reveal that carbonyl compounds with neighboring acid/base groups form hydrazones at accelerated rates. Similarly, tests of a hydrazine with a neighboring carboxylic acid group show that it also reacts at an accelerated rate. Rate constants for the fastest carbonyl/hydrazine combinations are 2-20 M-1 s-1, which is faster than recent strain-promoted cycloaddition reactions.
- Kool, Eric T.,Park, Do-Hyoung,Crisalli, Pete
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supporting information
p. 17663 - 17666
(2014/01/06)
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- Tri- and tetrasubstituted pyrazole derivates: Regioisomerism switches activity from p38MAP kinase to important cancer kinases
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In the course of searching for new p38α MAP kinase inhibitors, we found that the regioisomeric switch from 3-(4-fluorophenyl)-4-(pyridin-4-yl)-1- (aryl)-1H-pyrazol-5-amine to 4-(4-fluorophenyl)-3-(pyridin-4-yl)-1-(aryl)-1H- pyrazol-5-amine led to an almos
- Thaher, Bassam Abu,Arnsmann, Martina,Totzke, Frank,Ehlert, Jan E.,Kubbutat, Michael H. G.,Sch?chtele, Christoph,Zimmermann, Markus O.,Koch, Pierre,Boeckler, Frank M.,Laufer, Stefan A.
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supporting information; experimental part
p. 961 - 965
(2012/03/10)
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- Oxidation of 3-(3-or 4-pyridyl)-1,5-diphenylformazans in tetrazolium trichlorometallates: Structural and electrochemical investigation
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On interacting pyridine-containing formazans with cobalt(II) and copper(II) chlorides the richlorometallates of the corresponding cations are isolated, the structures of which were established by X-ray structural analysis. Using data of cyclic voltamperometry a scheme is proposed for the oxidation-reduction process of converting formazans into tetrazolium cations.
- Frolova,Vatsadze,Stash,Rakhimov,Zyk
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p. 1444 - 1456
(2008/09/21)
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- New C-arylation reaction found during a study on the interaction of aldohydrazones and arenediazonium chlorides
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The interaction of 2-pyridinecarboxaldehyde phenylhydrazone 1a with aryldiazonium chlorides furnished in complex mixtures, from which (E)-phenylhydrazones of 2-pyridylarylketones 3a-c were isolated as the main products.
- Frolova, Natalia A.,Vatsadze, Sergey Z.,Vetokhina, Natalia Yu.,Zavodnik, Valery E.,Zyk, Nikolay V.
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p. 251 - 254
(2007/10/03)
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- Kinetics and Mechanism for Pyridinecarboxaldehyde Phenylhydrazone Formation
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Phenylhydrazone formation from 4- and 3-pyridinecarboxaldehyde occurs with rate-determining carbinolamine dehydration under acidic, neutral, and basic conditions.Plots of first-order rate constants against amine concentration are nonlinear for these subst
- Moscovici, Riva,Okano, Valkiria,Amaral, Antonia T. do,Amaral, Luciano do
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p. 5157 - 5160
(2007/10/02)
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- Process for producing hydrazone derivatives of pyridinaldehydes
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An improved process for producing pyridinaldehydes and hydrazone derivatives thereof, for example, pyridinaldehyde-phenylhydrazones, is described. This comprises reacting a aminomethylpyridine with an aldehyde or a ketone to give a compound of the formula
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