Synthesis, Antimicrobial and Anticancer Activity of New Thiosemicarbazone Derivatives

Kulandaivelu, Umasankar; Padmini, Valisakka Gari; Suneetha, Kyatham; Boyapati, Shireesha; Vidyasagar, Jannu Vincent; Tadikonda, Rama Rao; Jayaveera, Κ. N.; Basu, Arijit; Jayaprakash, Venkatesan

doi:10.1002/ardp.201000201

Cited by 51 publications

(38 citation statements)

References 20 publications

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“…Series of fifteen (E)-Substituted-N-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)benzeneamine derivative (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) was aimed for the synthesis, following the three step procedure (Fig. 1).…”

Section: Resultsmentioning

confidence: 99%

“…In the second step the Schiff bases undergoes cyclization to yield pyrazole carboxaldehyde (b1-b5) nucleus by using dimethylformamide (DMF) and the desired compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) by the condensation reaction between pyrazole carboxaldehyde (b1-b5) and substituted amines in ethanol and drop of acetic acid under reflux. The prepared derivatives (a1-a5), (b1-b5) and (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) were then analyzed for structural confirmation by variety of analytical techniques such as FTIR, NMR, Mass Spectroscopy, Elemental analysis. The FTIR bands around 1590-1602 and 3190-3222 cm −1 due to the presence of C=N and NH functional groups confirmed the formation of compounds (a1-a5), the singlet around 1098-11.18 ppm in 1 H-NMR spectra due to the NH proton and a strong signal around 166.08-166.90 ppm in 13 C-NMR spectra due to C=N carbon further confirmed the formation of compounds (a1-a5).…”

Section: Resultsmentioning

confidence: 99%

“…The antimicrobial resistance (pathogens developed resistance to the available chemotherapeutic agents) has been a matter of great concern and reported the cause of 700,000 Deaths/Annum globally [1]. The pathogenic resistance has been a threat to the global community that once again become the major cause of the death due to the infectious disease [2]. To get rid off with this issue there is always requirement for the preparation of new chemotherapeutic agents to combat multi-drug resistant (MDR) strains.…”

Section: Introductionmentioning

confidence: 99%

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(E)-Substituted-N-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)benzeneamine: synthesis, characterization, antibacterial, and MTT assessment

et al. 2019

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To find out some novel antimicrobial chemotherapeutic agents, fifteen (E)-Substituted-N-(1,3-diphenyl-1H-pyrazol-4-yl) methylene)benzeneamine derivative (1-15) were synthesized. Structural elucidation of the prepared derivatives (1-15) was achieved by FTIR, NMR ( 1 H or 13 C), Mass spectroscopy and elemental analysis. After structural analyses the derivatives were subjected for biological assessment to estimate the antimicrobial therapeutic potential as well as the percent viability of the cells by disk diffusion methods and MTT assay. All the experiments were performed in triplicate; Ciprofloxacin and DMSO were used as positive and negative control. The results exhibited that the compounds 3, 4, 7-14 were found to exhibit significant antimicrobial therapeutic effect against all microorganisms, while some compounds of the series like 5, 6, 15, possessed moderate and compound 1 was found less significant potential. The percent viability of the cells were observed in the range 91-96% at lowest concentration 3.125 µM while 70-75% at the highest 100 µM.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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(E)-Substituted-N-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)benzeneamine: synthesis, characterization, antibacterial, and MTT assessment

et al. 2019

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“…Thiosemicarbazones (TSCs) constantly attract the interest of chemist and pharmacist because of their well-known and remarkable biological and pharmacological properties (antiviral, antibacterial or antitumoral activities); that is why the literature concerning these subjects is steadily increasing [1][2][3][4][5] . Such pharmacological activities are due to the strong chelating ability of these ligands with biologically important metal ions such as Fe 2+ , Cu 2+ , Ni 2+ and their reductive capacities 6,7 .…”

Section: Introductionmentioning

confidence: 99%

Crystal Structure and DFT Calculation Studies of Ni (II) Cinnamaldehyde Thiosemicarbazone Complex

2015

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Slow evaporation of a dilute DMSO solution of the title compound at room temperature, provided a brown crystal of Ni(CMTSC)2DMSO suitable for X-Rays study (space group: (5)). Two Ni atoms were located on special positions providing two molecules of Ni(CMTSC)2 different for their torsion angles and intermolecular interactions. In both molecules, the thiosemicarbazone coordinates as an anionic ligand via the thiosemicarbazone moiety's azomethine nitrogen and thiolatosulphur in a square-planar geometry. In the aim of investigating structural features, Density Functional Theory calculations of both ligand and complex were fully optimised with respect to the energy using B3LYP level. The predicted geometry parameters are compared with their corresponding X-ray crystallographic data.

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“…Kulandaivelu et al [9] , respectively. Although thiosemicarbazone has good antibacterial activity, it has great toxicity, which limits its application to a great extent.…”

Section: Introductionmentioning

confidence: 99%

Study on the Antimicrobial Activity of C3,6- Dibenzoylated Phenyl-Thiosemicarbazone-Chitosan Derivatives

Liu¹,

Zhong²

2017

Pharm Anal Chem

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The inhibitory effects of ten C 3,6 -dibenzoylated phenyl-thiosemicarbazone-chitosan derivatives on four species of animal pathogenic bacteria and four kinds of plant pathogenic fungi were studied. The antimicrobial activity of all derivatives is superior to that of raw chitosan. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the derivatives against Escherichia coli were 7.40 µg·mL -1 and 14.80 µg·mL -1 respectively. The bacteriostatic effect of derivative on Gram-negative bacteria is stronger. All of the derivatives had a certain antifungal effect on the tested fungi in the concentration range of 0.05 mg·mL -1 -2 mg·mL -1 , with a maximum inhibition index of 100%. The antimicrobial action of the derivatives increased with the increase of concentration.

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Synthesis, Antimicrobial and Anticancer Activity of New Thiosemicarbazone Derivatives

Cited by 51 publications

References 20 publications

(E)-Substituted-N-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)benzeneamine: synthesis, characterization, antibacterial, and MTT assessment

(E)-Substituted-N-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)benzeneamine: synthesis, characterization, antibacterial, and MTT assessment

Crystal Structure and DFT Calculation Studies of Ni (II) Cinnamaldehyde Thiosemicarbazone Complex

Study on the Antimicrobial Activity of C3,6- Dibenzoylated Phenyl-Thiosemicarbazone-Chitosan Derivatives

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