Design and Synthesis of Novel Benzopyran-2-one Derivatives of Expected Antimicrobial Activity through DNA Gyrase-B Inhibition

2008 ◽  
Vol 341 (11) ◽  
pp. 725-733 ◽  
Author(s):  
Ghaneya S. Hassan ◽  
Nahla A. Farag ◽  
Gehan H. Hegazy ◽  
Reem K. Arafa
Keyword(s):  
Antimicrobial Activity ◽  
Dna Gyrase ◽  
Design And Synthesis ◽  
Derivatives Of

ChemInform Abstract: Synthesis and Antimicrobial Activity of DNA-Gyrase Inhibiting Derivatives of 4-Oxo-1,4-dihydro-3-pyridinecarboxylic Acid.

ChemInform ◽  
2010 ◽  
Vol 25 (12) ◽  
pp. no-no
Author(s):  
C. BASSINI ◽  
C. BISMARA ◽  
R. CARLESSO ◽  
A. FERIANI ◽  
G. GAVIRAGHI ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Dna Gyrase ◽  
Pyridinecarboxylic Acid ◽  
Derivatives Of

Design and Synthesis of (E)-4-(2-Phenyl-2H-chromen-3-yl)but-3-en-2-ones and Evaluation of their In Vitro Antimicrobial Activity

2015 ◽  
Vol 12 (5) ◽  
pp. 352-358 ◽  
Author(s):  
Sabita Nayak ◽  
Subhendu Chakroborty ◽  
Sujitlal Bhakta ◽  
Pravati Panda ◽  
Seetaram Mohapatra ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Design And Synthesis

QSAR Analysis of Selected Antimicrobial Structures Belonging to Nitro-derivatives of Heterocyclic Compounds

2020 ◽  
Vol 17 (2) ◽  
pp. 214-225 ◽  
Author(s):  
Piotr Kawczak ◽  
Leszek Bober ◽  
Tomasz Bączek
Keyword(s):  
Antimicrobial Activity ◽  
Heterocyclic Compounds ◽  
Molecular Descriptors ◽  
Microbiological Activity ◽  
Activity Data ◽  
Qsar Analysis ◽  
Qsar Models ◽  
Nitro Derivatives ◽  
Semi Empirical ◽  
Derivatives Of

Background: Nitro-derivatives of heterocyclic compounds were used as active agents against pathogenic microorganisms. A set of 4- and 5-nitroimidazole derivatives exhibiting antimicrobial activity was analyzed with the use of Quantitative Structure-Activity Relationships (QSAR) method. The study included compounds used both in documented treatment and those described as experimental. Objective: The purpose of this study was to demonstrate the common and differentiating characteristics of the above-mentioned chemical compounds alike physicochemically as well as pharmacologically based on the quantum chemical calculations and microbiological activity data. Methods: During the study PCA and MLR analysis were performed, as the types of proposed chemometric approach. The semi-empirical and ab initio level of in silico molecular modeling was performed for calculations of molecular descriptors. Results: QSAR models were proposed based on chosen descriptors. The relationship between the nitro-derivatives structure and microbiological activity data was able to class and describe the antimicrobial activity with the use of statistically significant molecular descriptors. Conclusion: The applied chemometric approaches revealed the influential features of the tested structures responsible for the antimicrobial activity of studied nitro-derivatives.

scholarly journals Exonuclease VII repairs quinolone-induced damage by resolving DNA gyrase cleavage complexes

2021 ◽  
Vol 7 (10) ◽  
pp. eabe0384
Author(s):  
Shar-yin N. Huang ◽  
Stephanie A. Michaels ◽  
Brianna B. Mitchell ◽  
Nadim Majdalani ◽  
Arnaud Vanden Broeck ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Biology ◽  
Excision Repair ◽  
Dna Gyrase ◽  
Nuclease Activity ◽  
Bacterial Strains ◽  
Functional Importance ◽  
Quinolone Antibiotics ◽  
Repair Pathways ◽  
Exonuclease Vii

The widely used quinolone antibiotics act by trapping prokaryotic type IIA topoisomerases, resulting in irreversible topoisomerase cleavage complexes (TOPcc). Whereas the excision repair pathways of TOPcc in eukaryotes have been extensively studied, it is not known whether equivalent repair pathways for prokaryotic TOPcc exist. By combining genetic, biochemical, and molecular biology approaches, we demonstrate that exonuclease VII (ExoVII) excises quinolone-induced trapped DNA gyrase, an essential prokaryotic type IIA topoisomerase. We show that ExoVII repairs trapped type IIA TOPcc and that ExoVII displays tyrosyl nuclease activity for the tyrosyl-DNA linkage on the 5′-DNA overhangs corresponding to trapped type IIA TOPcc. ExoVII-deficient bacteria fail to remove trapped DNA gyrase, consistent with their hypersensitivity to quinolones. We also identify an ExoVII inhibitor that synergizes with the antimicrobial activity of quinolones, including in quinolone-resistant bacterial strains, further demonstrating the functional importance of ExoVII for the repair of type IIA TOPcc.

Design and Synthesis of Novel 20(S)-α-aminophosphonate Derivatives of Camptothecin as Potent Antitumor Agents

2021 ◽  
pp. 105065
Author(s):  
Yu-Yuan Chen ◽  
Yin-Peng Bai ◽  
Bin Li ◽  
Xiao-Bo Zhao ◽  
Cheng-Jie Yang ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Design And Synthesis ◽  
Derivatives Of

scholarly journals Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

2021 ◽  
Vol 11 (3) ◽  
pp. 1180
Author(s):  
Kinga Paruch ◽  
Łukasz Popiołek ◽  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Malm ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acid ◽  
Bacterial Infections ◽  
Acid Hydrazide ◽  
Antimicrobial Effect ◽  
In Vitro Antimicrobial Activity ◽  
Research Goal ◽  
New Compounds ◽  
Derivatives Of

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

scholarly journals Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors

Antibiotics ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 162
Author(s):  
Ahmed Ragab ◽  
Sawsan A. Fouad ◽  
Ola A. Abu Ali ◽  
Entsar M. Ahmed ◽  
Abeer M. Ali ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Fungal Growth ◽  
Dna Gyrase ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Dhfr Inhibitors ◽  
Positive Controls

Herein, a series of novel hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a–d, pyridine-2-one 3–10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis. All the synthesized compounds showed moderate to good antimicrobial activity against eight pathogens. The most promising six derivatives, 2a, 2b, 2d, 3a, 8, and 11, revealed to be best in inhibiting bacterial and fungal growth, thus showing bactericidal and fungicidal activity. These derivatives exhibited moderate to potent inhibition against DNA gyrase and DHFR enzymes, with three derivatives 2d, 3a, and 2a demonstrating inhibition of DNA gyrase, with IC50 values of 18.17–23.87 µM, and of DHFR, with IC50 values of 4.33–5.54 µM; their potency is near to that of the positive controls. Further, the six derivatives exhibited immunomodulatory potential and three derivatives, 2d, 8, and 11, were selected for further study and displayed an increase in spleen and thymus weight and enhanced the activation of CD4+ and CD8+ T lymphocytes. Finally, molecular docking and some AMED studies were performed.

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