Synthesis and Antimicrobial Activity of New 1,3-Thiazolidin-4-one Derivatives Obtained from Carboxylic Acid Hydrazides

Popiołek, Łukasz; Biernasiuk, Anna; Malm, Anna

doi:10.1080/10426507.2014.919293

Cited by 33 publications

(38 citation statements)

References 22 publications

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“…Appropriate DMSO, growth and sterile controls were carried out. The medium with no tested substances was used as control 28,29 . The minimal bactericidal concentration (MBC) or minimal fungicidal concentration (MFC) is defined as the lowest concentration of the compounds that is required to kill a particular bacterial or fungal species.…”

Section: In Vitro Antimicrobial Assaymentioning

confidence: 99%

Hydrazide-hydrazones of 3-methoxybenzoic acid and 4-tert-butylbenzoic acid with promising antibacterial activity against Bacillus spp

Popiołek¹,

Biernasiuk

2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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A series of 28 hydrazide-hydrazones of 3-methoxybenzoic and 4-tert-butylbenzoic acid were synthesized and screened in vitro against the panel of reference strains of bacteria and fungi with the use of the broth microdilution method according to EUCAST and CLSI guidelines. Five of the synthesized compounds were found to exhibit high bacteriostatic or bactericidal activity against Gram-positive bacteria. The antimicrobial activity of compounds 13, 14, and 16 against Bacillus spp. was higher than that of commonly used antibiotics, like cefuroxime or ampicillin.

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Section: In Vitro Antimicrobial Assaymentioning

confidence: 99%

Hydrazide-hydrazones of 3-methoxybenzoic acid and 4-tert-butylbenzoic acid with promising antibacterial activity against Bacillus spp

Popiołek¹,

Biernasiuk

2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…The lowest compound concentrations with no visible growth observed were assessed as a bactericidal/ fungicidal concentration. All the experiments were repeated three times and representative data are presented in Tables 2 and 3 [19][20][21] . In this study, no bioactivity was defined as a MIC41000 mg/mL, mild bioactivity as a MIC in the range 501-1000 mg/mL, moderate bioactivity with MIC from 126 to 500 mg/mL, good bioactivity as a MIC in the range 26-125 mg/mL, strong bioactivity with MIC between 10 and 25 mg/mL and very strong bioactivity as a MIC 510 mg/mL.…”

Section: Antibacterial and Antifungal Activity Assessmentmentioning

confidence: 99%

“…The medium without tested substances was used as a control [19][20][21] . The MBC (Minimal Bactericidal Concentration) or MFC (Minimal Fungicidal Concentration) are defined as the lowest concentration of the compounds that is required to kill a particular bacterial or fungal species.…”

Section: Antibacterial and Antifungal Activity Assessmentmentioning

confidence: 99%

“…The inhibition of microorganisms growth was judged by comparing with a control culture prepared without any sample tested. Ciprofloxacin, vancomycin and fluconazole (Sigma-Aldrich, St. Louis, MO) were used as a reference antibacterial or antifungal compounds, respectively [19][20][21] . Subsequently, minimal inhibitory concentration (MIC) of the compounds was examined by the microdilution broth method, using their two-fold dilutions in Mueller-Hinton broth or Mueller-Hinton broth with 5% sheep blood (for bacteria) and RPMI 1640 broth with MOPS (for fungi) prepared in 96-well polystyrene plates.…”

Section: Antibacterial and Antifungal Activity Assessmentmentioning

confidence: 99%

“…All the synthesized compounds were in vitro screened for their antibacterial and antifungal activities using a broth microdilution method according to European Committee on Antimicrobial Susceptibility Testing (EUCAST) 19 and Clinical and Laboratory Standards Institute guidelines (CLSI) 20 [19][20][21] . Samples containing 5 mg, 1 mg or 0.5 mg of tested compounds A1-A7 were dissolved in 1 mL of DMSO.…”

Section: Antibacterial and Antifungal Activity Assessmentmentioning

confidence: 99%

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Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes

Boguszewska-Czubara

Łapczuk-Krygier

Rykala

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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(2016) Novel synthesis scheme and invitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes, Journal of Enzyme Inhibition and Medicinal Chemistry, 31:6, 900-907, DOI: 10.3109/14756366.2015 AbstractDrug resistance has become a major concern in the field of infection management, therefore searching for new antibacterial agents is getting more challenging. Our study presents an optimized and eco-friendly synthesis scheme for a panel of nitroalkenes bearing various functional groups in the aromatic moiety and bromine or cyano substituents in 1 position of nitrovinyl moiety. The presence of nitrolefine group outside the ring minimalizes genotoxic properties while conjugation of aryl group with nitrovinyl moiety increases stability of the compounds. Then our research focused on evaluation of biological properties of such obtained (E)-2-aryl-1-cyano-1-nitroethenes. As they exhibit strong bacteriostatic and bactericidal activities against reference bacteria and yeast species with no detectable cytotoxicity towards cultured human HepG2 and HaCaT cells, they could be promising candidates for the replacement of traditional nitrofurane-containing antibacterial drugs. Nevertheless, validation of the obtained data in an in vivo model and additional safety studies on mutagenicity are still required.

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New Hydrazides and Hydrazide‐Hydrazones of 2,3‐Dihalogen Substituted Propionic Acids: Synthesis and in vitro Antimicrobial Activity Evaluation

Popiołek¹,

Biernasiuk²

2017

Chemistry & Biodiversity

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The main aim of this research was the synthesis, spectral identification and in vitro antimicrobial evaluation of new hydrazides and hydrazide-hydrazones of 2,3-dihalogen substituted propionic acids. New hydrazides were obtained by the substitution reaction of appropriate ethyl esters of 2,3-dihalogen substituted propionic acids with hydrazine hydrate. Then obtained hydrazides were subjected to condensation reaction with various aldehydes which yielded with new hydrazide-hydrazone derivatives. All obtained compounds were identified on the basis of spectral methods ( H-NMR, C-NMR) and in vitro screened against a panel of bacterial and fungal strains according to EUCAST and CLSI guidelines.

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Synthesis and Antimicrobial Activity of New 1,3-Thiazolidin-4-one Derivatives Obtained from Carboxylic Acid Hydrazides

Cited by 33 publications

References 22 publications

Hydrazide-hydrazones of 3-methoxybenzoic acid and 4-tert-butylbenzoic acid with promising antibacterial activity against Bacillus spp

Hydrazide-hydrazones of 3-methoxybenzoic acid and 4-tert-butylbenzoic acid with promising antibacterial activity against Bacillus spp

Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes

New Hydrazides and Hydrazide‐Hydrazones of 2,3‐Dihalogen Substituted Propionic Acids: Synthesis and in vitro Antimicrobial Activity Evaluation

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