scholarly journals Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains

2018 ◽  
Vol 143 ◽  
pp. 1474-1488 ◽  
Author(s):  
Ilija N. Cvijetić ◽  
Tatjana Ž. Verbić ◽  
Pedro Ernesto de Resende ◽  
Paul Stapleton ◽  
Simon Gibbons ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Multidrug Resistant ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of 5′-C-piperidinyl-5′-O-aminoribosyluridines as potential antibacterial agents

2015 ◽  
Vol 13 (28) ◽  
pp. 7720-7735 ◽  
Author(s):  
Takeshi Nakaya ◽  
Akira Matsuda ◽  
Satoshi Ichikawa
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Human Cells ◽  
Ritter Reaction ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Caprazamycin analogues, which were designed and synthesized via an aza-Prins–Ritter reaction, exhibit a good MraY and antibacterial activity without cytotoxicity against human cells.

scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Synthesis And Biological Evaluation

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

scholarly journals Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents

MedChemComm ◽  
2018 ◽  
Vol 9 (8) ◽  
pp. 1293-1304 ◽  
Author(s):  
Niu-niu Zhang ◽  
Zhi-yong Liu ◽  
Jie Liang ◽  
Yun-xiang Tang ◽  
Lu Qian ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Biological Evaluation ◽  
Antitubercular Agents ◽  
Design Synthesis ◽  
New Class ◽  
Synthesis And Biological Evaluation

m-Amidophenol derivatives were found to potently inhibit the growth of M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains.

scholarly journals Design, Synthesis and Biological Evaluation of New Piperazin-4-yl-(acetyl-thiazolidine-2,4-dione) Norfloxacin Analogues as Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3959 ◽  
Author(s):  
Marc ◽  
Araniciu ◽  
Oniga ◽  
Vlase ◽  
Pîrnău ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Binding Mode ◽  
Biological Properties ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Parent Molecule ◽  
Synthesis And Biological Evaluation

 In an effort to improve the antimicrobial activity of norfloxacin, a series of hybrid norfloxacin–thiazolidinedione molecules were synthesized and screened for their direct antimicrobial activity and their anti-biofilm properties. The new hybrids were intended to have a new binding mode to DNA gyrase, that will allow for a more potent antibacterial effect, and for activity against current quinolone-resistant bacterial strains. Moreover, the thiazolidinedione moiety aimed to include additional anti-pathogenicity by preventing biofilm formation. The resulting compounds showed promising direct activity against Gram-negative strains, and anti-biofilm activity against Gram-positive strains. Docking studies and ADMET were also used in order to explain the biological properties and revealed some potential advantages over the parent molecule norfloxacin.

scholarly journals Synthesis and Biological Evaluation of 7-O-Modified Formononetin Derivatives

2008 ◽  
Vol 2008 ◽  
pp. 1-4 ◽  
Author(s):  
Ying Yang ◽  
Wen-Jun Mao ◽  
Huan-Qiu Li ◽  
Tao-Tao Zhu ◽  
Lei Shi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cell Line ◽  
Jurkat Cell ◽  
Preliminary Investigation ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Chemical Structures ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation ◽  
Antiproliferative Activities

Three series of novel formononetin derivatives were synthesized, in which formononetin and heterocyclic moieties were separated by 2-carbon, 3-carbon, and 4-carbon spacers. The chemical structures of these compounds were confirmed. All the derivatives were screened for antiproliferative activities against Jurkat cell line and HepG-2 cell line. In this paper, compounds prepared were also screened for their antibacterial activity of six bacterial strains. Compound 3b exihibited promising antibacterial activity against B. subtilis with minimal inhibitory concentration (MIC) value of 0.78 μg/mL, and compound 5e showed significant antiproliferative activities against Jurkat cell growth with IC50 of 1.35×10−4 μg/mL. The preliminary investigation of structure-activity relationships (SARs) was also discussed based on the obtained experimental data.

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