A Convenient Synthesis of new Phenanthrolinone and Naphthyridinone Derivatives: Evaluation of their Biological activity

2014 ◽  
Vol 9 (1) ◽  
pp. 1866-1872
Author(s):  
Mona A. Hosny ◽  
Wafaa A. Mokbel ◽  
Emtithal A. El-Sawi

A novel and effective synthesis of substituted acetamide via smiles rearrangement is described. Treatment of phenols with 2-chloroacetamide in the presence of sodium hydroxide and DMA where substituted phenols, which contain electron withdrawing groups, are more reactive for smiles rearrangement. The reaction followed by cyclization of the product by E.A.A. afforded the corresponding substituted phenanthrolinone and naphthyridinone in good yields and showed higher activity against (G- and G+, Eschierchia coli and Staphylococcus aureus respectively) and good activity toward Aspergillius flavus and Candida albicans.


2013 ◽  
Vol 9 (1) ◽  
pp. 1866-1872
Author(s):  
Mona A. Hosny ◽  
Wafaa A. Mokbel ◽  
Emtithal A. El-Sawi

A novel and effective synthesis of substituted acetamide via smiles rearrangement is described. Treatment of phenols with 2-chloroacetamide in the presence of sodium hydroxide and DMA where substituted phenols, which contain electron withdrawing groups, are more reactive for smiles rearrangement. The reaction followed by cyclization of the product by E.A.A. afforded the corresponding substituted phenanthrolinone and naphthyridinone in good yields and showed higher activity against (G- and G+, Eschierchia coli and Staphylococcus aureus respectively) and good activity toward Aspergillius flavus and Candida albicans.



2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Author(s):  
Madalina Mihalache ◽  
Cornelia Guran ◽  
Aurelia Meghea ◽  
Vasile Bercu ◽  
Ludmila Motelica ◽  
...  

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: [Cu(TB)(HA)]Cl (C1), [Cu(TB)(HA)CH3COO]�H2O (C2) and [Cu(TB)(HA)](NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications.









2002 ◽  
Vol 8 (5) ◽  
pp. 269-274 ◽  
Author(s):  
V. Zelenák ◽  
K. Györyová ◽  
D. Mlynarcík

The antibacterial and antifungal activity of zinc(II) carboxylates with composition Zn(RCOO)2•nH2O(R =H-, CH3− , CH3CH2CH2- , (CH3)2CH- , XCH2- , X=Cl, Br, I, n=0 or 2), [ZnX2(Nia+CH2COO-)2] (Nia=nicotinamide, X=Cl, Br, I) and [Zn(XCH2COO)2(Caf)2]•2H2O (Car=caffeine, X=Cl, Br) is studied against bacterial strains Staphylococcus aureus, Escherichia coli and yeast Candida albicans. The structural types are assigned to the prepared compounds and the influence of (i) carboxylate chain length, (ii) substitution of hydrogen atom of carboxylate by halogen and (iii) presence of N-donor organic ligands on the biological activity is discussed.



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