Synthesis and characterization of novel dimerics-triazine derivatives as potential anti-bacterial agents against MDR clinical isolates

2018 ◽  
Vol 42 (13) ◽  
pp. 10676-10688 ◽  
Author(s):  
Doaa R. Ramadan ◽  
Aly A. Elbardan ◽  
Adnan A. Bekhit ◽  
Ayman El-Faham ◽  
Sherine N. Khattab
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Bases ◽  
Mammalian Cells ◽  
High Selectivity ◽  
Bacterial Activity ◽  
Selectivity Index ◽  
Synthesis And Characterization ◽  
Triazine Derivatives ◽  
Ampicillin Trihydrate

Several dimerics-triazine Schiff bases displayed more potent anti-bacterial activity compared with ampicillin trihydrate. They revealed significantly low MIC values towards the tested MDR strains and showed a high selectivity index towards antimicrobial activity againstK. pneumoniaeandMRSA1compared to mammalian cells.

SYNTHESIS AND CHARACTERIZATION OF SOME SCHIFF BASES BASED ON 1, 8-DIAMINOOCTANE FOR EVALUATION AS CORROSION INHIBITORS

2018 ◽  
Vol 42 (1) ◽  
pp. 1-29
Author(s):  
Hashem, A. I. ◽  
Ismaeel, H. S. ◽  
Dawood, E. A. ◽  
and El-Mokadem, T. H.
Keyword(s):  
Schiff Bases ◽  
Corrosion Inhibitors ◽  
Synthesis And Characterization

DESIGN, SYNTHESIS, AND CHARACTERIZATION OF THE SOME NOVEL 2‐AMINO-PYRIDINE‐3‐ CARBONITRILE AND 2‐AMINO-4H-PYRAN‐3‐CARBONITRILE DERIVATIVES AGAINST ANTIMICROBIAL ACTIVITY AND ANTIOXIDANT ACTIVITY

2020 ◽  
pp. 125-134
Author(s):  
SURENDRA BABU LAGU ◽  
RAJENDRA PRASAD YEJELLA
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Synthesis And Characterization ◽  
Zone Of Inhibition ◽  
Design Synthesis ◽  
Instrumental Methods ◽  
Objective Investigation

Objective: Investigation, the series of newer 2‐amino-pyridine‐3‐carbonitrile and 2‐amino-4H-pyran‐3‐carbonitrile derivative were synthesized and evaluated antimicrobial activities and antioxidant activity. Methods: Novel synthesized chalcones were further condensation to give 2-amino-3-cyanopyridine and 2-amino-3-cyanopyrans in the presence of malononitrile, pyridine, and ammonia acetate. The product is characterized by conventional and instrumental methods. Pyridine and 4-H-Pyran and their analogs occupy prime position due to their diverse applications. Results: The compounds A3C and B3C exhibited marked zone of inhibition with 30.02±0.02 mm and 29.06±0.01 mm, respectively. Docking studies suggested possible interactions with dihydrofolic reductase 4 with 9.15 and −9.67 kcal/mol, respectively. The IC50 30.28±0.01 exhibited A3C by 2,2-diphenylpicrylhydrazyl methods which is better among the series. The 2-amino-3-cyanopyridine derivatives were found good activity than 2-amino-3-cyanopyrane derivative. Among all synthesized compounds few having potent activity and some are near to the standard. Conclusion: Antimicrobial activity and antioxidant of the newly synthesized pyrans and pyridines derivatives will definitely inspire future researchers for the preparation of new analogs.

scholarly journals Diversity Focused Semisyntheses of Tetronate Polyether Ionophores

2019 ◽  
Author(s):  
Shaoquan Lin ◽  
Han Liu ◽  
Esben B. Svenningsen ◽  
Christine Pedersen ◽  
Peter Nørby ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cancer Cells ◽  
Mammalian Cells ◽  
Biological Activities ◽  
Structural Diversity ◽  
Bacterial Activity ◽  
Cation Binding ◽  
Detailed Understanding ◽  
Structure Activity ◽  
Aggressive Cancer

The polyether ionophores are complex natural products capable of transporting cations across biological membranes. Many family members possess highly potent antimicrobial activity and a few selected compounds have ability to target particularly aggressive cancer cells. Despite these interesting perspectives, a detailed understanding of the cellular mode-of-action of polyether ionophores is generally lacking. In principle, broad mapping of structure-activity relationships across several biological activities could provide mechanistic insights as well as identification of lead structures but access to structural diversity within the overall class is synthetically very challenging. In this manuscript, we demonstrate that novel polyether ionophores can be constructed by recycling components of highly abundant polyethers. We provide the first examples of synthetically incorporating halogen-functionalized tetronic acids as cation-binding groups into polyether ionophores and we identify analogs with strong anti-bacterial activity and minimal effects on mammalian cells.

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