Benzaldehyde thiosemicarbazone derivatives against replicating and nonreplicating Mycobacterium tuberculosis

Volynets, Galyna P.; Tukalo, M. A.; Bdzhola, Volodymyr G.; Derkach, N. M.; Gumeniuk, Mykola; Tarnavskiy, S. S.; Starosyla, Sergiy A.; Yarmoluk, S. M.

doi:10.1038/s41429-019-0140-9

Cited by 17 publications

(15 citation statements)

References 31 publications

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“…The higher the hydrophobic interaction, the lower the hydrogen bond interaction and vice versa. Our findings are similar to that of the experimental studies carried out by Volynets et al [ 24 ]. The in vitro studies on benzaldehyde thiosemicarbazone derivatives against M. tuberculosis results in the minimal inhibitory concentration (MIC) of 0.68 μ M for compound 13 and 0.74 μ M for compound 20.…”

Section: Resultssupporting

confidence: 94%

“…In the recent study, Volynets et al, in 2019, have experimentally proved the activity of benzaldehyde thiosemicarbazone against M. tuberculosis . Hence, in the present study, we have retrieved the synthesized benzaldehyde thiosemicarbazone derivatives from the literature and screened against one of the main target DNA gyrases to find a potential inhibitor for M. tuberculosis [ 24 ] through molecular modelling methods. Our study may give an idea to the researchers who are designing drug against M. tuberculosis in the molecular level.…”

Section: Introductionmentioning

confidence: 99%

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Structure-Based Virtual Screening of Benzaldehyde Thiosemicarbazone Derivatives against DNA Gyrase B of Mycobacterium tuberculosis

Kistan¹,

Benedict²,

Vasanthan³

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Emergence of antibiotic-resistant Mycobacterium tuberculosis (M. tuberculosis) restricts the availability of drugs for the treatment of tuberculosis, which leads to the increased morbidity and mortality of the disease worldwide. There are many intrinsic and extrinsic factors that have been reported for the resistance mechanism. To overcome such mechanisms, chemically synthesized benzaldehyde thiosemicarbazone derivatives were screened against M. tuberculosis to find potential inhibitor for tuberculosis. Such filtering process resulted in compound 13, compound 21, and compound 20 as the best binding energy compounds against DNA gyrase B, an important protein in the replication process. The ADMET prediction has shown the oral bioavailability of the novel compounds.

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Section: Resultssupporting

confidence: 94%

Section: Introductionmentioning

confidence: 99%

Structure-Based Virtual Screening of Benzaldehyde Thiosemicarbazone Derivatives against DNA Gyrase B of Mycobacterium tuberculosis

Kistan¹,

Benedict²,

Vasanthan³

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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“…Thiosemicarbazones (TSCs) and their metal complexes are versatile molecules with a wide spectrum of antimicrobial, antitrypanosomal, antitumor, antimalarial, and antiviral activities and have been studied intensely in pharmaceutical and medicinal chemistry [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 , 13 ]. TSCs are able to block the genetic expression of wide variety of viruses [ 11 , 13 ], including the herpes simplex virus [ 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 ].…”

Section: Introductionmentioning

confidence: 99%

Characterization and Release Behavior of a Thiosemicarbazone from Electrospun Polyvinyl Alcohol Core-Shell Nanofibers

et al. 2020

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Mats of polyvinyl alcohol (PVA) core–shell nanofibers were produced using coaxial electrospinning in the presence of a thiosemicarbazone (TSC) N4-(S)-1-phenylethyl)-2-(pyridin-2-yl-ethylidene)hydrazine-1-carbothioamide (HapyTSCmB). Monolithic fibers with 0% or 5% TSC and core–shell fibers with 10% TSC in the spinning solution were studied to compare stability and release rates. SEM showed the formation of uniform, bead-free, cylindrical, and smooth fibers. NMR spectroscopy and thermal analysis (TG/DTA) gave proof for the chemical integrity of the TSC in the fiber mats after the electrospinning process. Attenuated total reflection Fourier-transform infrared (ATR-FTIR) spectroscopy showed no TSC on the surface of the PVA/TSC-PVA fibers confirming the core–shell character. The TSC release profiles of the fibers as studied using UV-vis absorption spectroscopy showed a slower release from the PVA/TSC-PVA core–shell structure compared with the monolithic PVA/TSC fibers as well as lower cumulative release percentage (17%). Out of several release models, the Korsmeyer–Peppas model gave the best fit to the experimental data. The main release phase can be described with a Fick-type diffusion mechanism. Antibacterial properties were tested against the Gram-positive Staphylococcus aureus bacterium and gave a minimal inhibitory concentration of 12.5 μg/mL. 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT)-based cytotoxicity experiments showed that the cell viability of fibroblast at different contents of TSC was slightly decreased from 1.5% up to 3.5% when compared to control cells.

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“…Salicylaldehyde thiosemicarbazone ligand complex with copper have showed good resistant, in vitro, against colon carcinoma, melanoma, pancreatic adenocarcinoma, thyroid carcinoma, and ovarian carcinoma [6]. Some benzaldehyde thiosemicarbazone derivatives demonstrate antimycobacterial activity, under hypoxia, against M. tuberculosis [7]. Palladium (II) salicylaldiminato thiosemicarbazone complexes showed an amazing antiprotozoal activity on metronidazole resistant Trichomonas vaginalis [8].…”

Section: Introductionmentioning

confidence: 99%

Solvent free synthesis of hydrazine carbothioamide derivatives as a precursor in the preparation of new mononuclear Mn(II), Cu(II), and Zn(II) complexes: Spectroscopic characterizations

Al‐Hazmi¹,

Saad²,

Alosaimi³

et al. 2021

Bull. Chem. Soc. Eth.

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ABSTRACT. Over the last few years considerable attention has been devoted to the study of Schiff base complexes of metal(II) containing nitrogen, oxygen and sulfur donor ligands due to their diverse biological activities. Therefore, the Schiff base thiosemicarbazone derivatives of 2-(2-hydroxy-3-methoxybenzylidene) hydrazine carbothioamide (HL1) and 2-(4-bromo-2-hydroxy-3-methoxybenzylidene) hydrazine carbothioamide (HL2) were synthesized with solvent free technique using silica gel as material support for the reaction. The structures of the precursor’s organic products confirmed with their 1H, 13C NMR, IR and microanalysis data. Six new manganese(II), copper(II), and zinc(II) complexes of HL1 and HL2 2-(2-hydroxy-3-methoxybenzylidene) hydrazinecarbothioamide derivatives with the general formulation [ML1Cl] and [ML2Cl], where M = Mn2+, Cu2+, and Zn2+ were prepared and well discussed by using elemental analyses, magnetic moments, molar conductance, infrared and electronic spectral techniques. The assignments data of spectroscopic analysis confirm that the synthesized thiosemicarbazone Schiff bases of acts as a tridentate ligand as sulfur-oxygen-nitrogen donating atoms. The values of magnetic moments agreed with the data of electronic spectra which both suggested a four-coordination geometry of the synthesized complexes. KEY WORDS: Schiff base, Thiosemicarbazone, Manganese(II) complex, Copper(II) complex, Zinc(II) complex Bull. Chem. Soc. Ethiop. 2021, 35(2), 413-424. DOI: https://dx.doi.org/10.4314/bcse.v35i2.14

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Benzaldehyde thiosemicarbazone derivatives against replicating and nonreplicating Mycobacterium tuberculosis

Cited by 17 publications

References 31 publications

Structure-Based Virtual Screening of Benzaldehyde Thiosemicarbazone Derivatives against DNA Gyrase B of Mycobacterium tuberculosis

Structure-Based Virtual Screening of Benzaldehyde Thiosemicarbazone Derivatives against DNA Gyrase B of Mycobacterium tuberculosis

Characterization and Release Behavior of a Thiosemicarbazone from Electrospun Polyvinyl Alcohol Core-Shell Nanofibers

Solvent free synthesis of hydrazine carbothioamide derivatives as a precursor in the preparation of new mononuclear Mn(II), Cu(II), and Zn(II) complexes: Spectroscopic characterizations

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