Synthesis and antibacterial activities of N-[(1-aryl-3-phenyl-pyrazol-4-yl)methylene]-2-(halo-o-hydroxyphenyl)hydrazide derivatives

Ya, Liu; Lu, Bo-Wei; Lu, Junrui; Chun-Wei, Xin; Li, Jianfa; Mu, Jiangbei; Xiu-rong, Bao

doi:10.1007/s40242-013-2491-2

Cited by 6 publications

(4 citation statements)

References 17 publications

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“…According to literatures [25,26], entecavir, control group and compounds 5a-5l cell culture fluids(4 nmol/mL) were prepared, respectively. Each kind of culture fluid was used to culture HepG2.2.15 cells(transfected by HBV) about 72 h in vitro.…”

Section: Hbv Dna Inhibition Efficacy Assaymentioning

confidence: 99%

RETRACTED ARTICLE: Synthesis and biological evaluation of entecavir 4′-ester derivatives

Feng

Liu

Liang

et al. 2014

Chem. Res. Chin. Univ.

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Entecavir can significantly inhibit the replication of HBV-DNA, reduce the HBV-DNA level in blood serum. But suffering from low oral bioavailability, entecavir has low intestinal membrane permeability and poor metabolic stability. In this study, 12 different derivatives of entecavir 4'-ester were regioselectively synthesized and their apical-to-basolateral permeabilities across Caco-2 cells and HBV-DNA inhibitory efficacies were evaluated. Most of the compounds showed high permeabilities across Caco-2 cells compared with entecavir, compounds 5b and 5e also exhibited comparable anti-HBV activities with that of entecavir, especially.

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Section: Hbv Dna Inhibition Efficacy Assaymentioning

confidence: 99%

RETRACTED ARTICLE: Synthesis and biological evaluation of entecavir 4′-ester derivatives

Feng

Liu

Liang

et al. 2014

Chem. Res. Chin. Univ.

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“…All deuterated solvents were purchased from Cambridge Isotope Laboratories. 3-Bromobenzohydrazide ( 3.0 ), 4-bromobenzohydrazide ( 3.4 ), 2-hydroxy-5-bromobenzohydrazide ( 3.5 ), 2-hydroxy-3,5-dibromobenzohydrazide ( 3.6 ), 3-quinolinecarbohydrazide ( 3.7 ), 3,5-dibromobenzohydrazide ( 3.9 ), 4-cyanobenzohydrazide ( 3.11 ), 4-trifluoromethylbenzohydrazide ( 3.13 ), 4-fluorobenzohydrazide ( 3.20 ), 4-aminobenzohydrazide (3.24) , 4-acetamidobenzohydrazide ( 3.26 ), 2-methylbenzohydrazide ( 3.27 ), and 2-benzyloxy-3,5-dibromobenzaldehyde ( 4.1 ) were synthesized by the literature methods.…”

Section: Methodsmentioning

confidence: 99%

SAR Studies on Aromatic Acylhydrazone-Based Inhibitors of Fungal Sphingolipid Synthesis as Next-Generation Antifungal Agents

et al. 2019

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Recently, the fungal sphingolipid glucosylceramide (GlcCer) synthesis has emerged as a highly promising new target for drug discovery of next-generation antifungal agents, and we found two aromatic acylhydrazones as effective inhibitors of GlcCer synthesis based on HTP screening. In the present work, we have designed libraries of new aromatic acylhydrazones, evaluated their antifungal activities (MIC80 and time-kill profile) against C. neoformans, and performed an extensive SAR study, which led to the identification of five promising lead compounds, exhibiting excellent fungicidal activities with very large selectivity index. Moreover, two compounds demonstrated broad spectrum antifungal activity against six other clinically relevant fungal strains. These five lead compounds were examined for their synergism/cooperativity with five clinical drugs against seven fungal strains, and very encouraging results were obtained; e.g., the combination of all five lead compounds with voriconazole exhibited either synergistic or additive effect to all seven fungal strains.

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“…Meanwhile, hydrazone, a highly efficient pharmacophore, has attracted more and more attention in the pesticides areas due to its broad-activities, such as antibacterial [ 19 ], fungicidal [ 20 , 21 ], insecticidal [ 20 , 22 , 23 ], and antiviral [ 20 , 24 ] activities. A few of the pyrazole-hydrazone derivatives have also been reported and possess various biological activities such as antibacterial [ 25 ], antifungal [ 21 ], anticancer [ 26 ], antioxidant [ 27 ], anti-inflammatory [ 28 ], antitumor and antiangiogenesis [ 29 ] and antiplatelet activities [ 30 ]. In addition, isoxazole, a five membered heterocyclic ring, was an important scaffold for synthesis of various natural compounds and their congeners and had a broad spectrum of pharmacological activities like antibacterial [ 31 ], antifungal [ 9 , 32 , 33 ], insecticide [ 34 , 35 ], and antiviral [ 36 ] activities.…”

Section: Introductionmentioning

confidence: 99%

Novel Pyrazole-Hydrazone Derivatives Containing an Isoxazole Moiety: Design, Synthesis, and Antiviral Activity

Yang

Gan

2018

Molecules

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In this study, a series of novel pyrazole-hydrazone derivatives containing an isoxazole moiety were synthesized. Antiviral bioassays indicated that some of the title compounds exhibited better in vivo antiviral activities against tobacco mosaic virus (TMV). In particular, compounds 6a, 6c and 6q exhibited the best curative activity, protection activity, and inactivation activity against TMV, respectively, which were superior to those of Ningnanmycin. This study demonstrated that this series of novel pyrazole-hydrazone derivatives containing an isoxazole amide moiety could effectively control TMV.

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Synthesis and antibacterial activities of N-[(1-aryl-3-phenyl-pyrazol-4-yl)methylene]-2-(halo-o-hydroxyphenyl)hydrazide derivatives

Cited by 6 publications

References 17 publications

RETRACTED ARTICLE: Synthesis and biological evaluation of entecavir 4′-ester derivatives

RETRACTED ARTICLE: Synthesis and biological evaluation of entecavir 4′-ester derivatives

SAR Studies on Aromatic Acylhydrazone-Based Inhibitors of Fungal Sphingolipid Synthesis as Next-Generation Antifungal Agents

Novel Pyrazole-Hydrazone Derivatives Containing an Isoxazole Moiety: Design, Synthesis, and Antiviral Activity

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