scholarly journals Synthesis, Characterization of Biologically Potent Novel Chalcones Bearing Urea, Thiourea and Acetamide Linkages

Author(s):  
Nirali S. Mewada ◽  
Dhruvin R. Shah ◽  
Kishor H. Chikhalia

Three series of some novel chalcone based urea, thiourea and acetamide derivatives were designed, synthesized and screened for their antimicrobial and antifungal activities. All the synthesized compounds are first reported. The structures of the compounds were elucidated with the aid of elemental analysis and spectral methods including IR, 1H-NMR spectral data. The prepared compounds were evaluated for antibacterial activity against two Gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus), two Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also investigated for their antifungal activity using the broth micro dilution method. The bioassay results showed that compounds a few compounds showed good to superior in vitro antibacterial and antifungal activity.

Author(s):  
Shraddha M. Prajapati ◽  
Rajesh H. Vekariya ◽  
Kinjal D. Patel ◽  
Shyamali N. Panchal ◽  
Hitesh D. Patel ◽  
...  

A library of quinoline analog two novel series of azetidin (SH1-5) and thiazolidin (SHa-e) derivatives were designed and synthesized with simple and eco-friendly methodologies. The structures of the compounds were elucidated with the aid of elemental analysis, IR, 1H-NMR and mass spectral data. These novel synthesized compounds were evaluated for antibacterial activity against two gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus) and two gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also studied for their antifungal activity with Candida albicans, Aspergillus niger, Aspergillus clavatus using the broth dilution technique. Most of the compounds were the best bio-active desired antibacterial analog with less MIC value against different tested strains.


Author(s):  
A. R. Chabukswar ◽  
P.V. Adsule ◽  
P.B. Randhave ◽  
Manini Mantri

We have designed and synthesized (Z)-2-(5-methyl-2-oxo-2H-chromen-7-yl) oxy)-N’-(2-oxoindolin-3-ylidin) acetohydrazide derivatives by reacting 7-hydroxy-4-methyl-coumarin and substituted isatin to afford 12 substituted coumarin acetohydrazide derivatives. The synthesized compounds of coumarin acetohydrazide derivatives were designed and evaluated to study for their possible interactions as DNA gyrase inhibitors. All the synthesized coumarin acetohydrazide compounds have been characterized by spectral analysis IR, 1H NMR and mass spectroscopy. The compounds have been evaluated for In vitro antibacterial and antifungal activity against S. aureus, B. subtilus, E. coli, P. aeruginosa and fungi C. albicans and A. niger. In case of Gram positive bacteria and Gram negative bacteria Compound P5C, M5C, C5C exhibited significant activity. Compounds P5N, M5N, C5N shown moderate activity. Compound P5C, M5C, C5C shown significant Antifungal activity against C. albicans and A. niger. Compounds P5C, M5C, C5C are found to exert significant antibacterial as well as antifungal activity and can serve as potential compound against infectious diseases in future.


2011 ◽  
Vol 11 (2) ◽  
pp. 148-153
Author(s):  
Hemant Panwar ◽  
Shishupal Singh

3-Aryl-5H,13aH-quinolino(3,2-f)(1,2,4)triazolo(4,3-b)(1,2-diaza-4-sulpho)azepines [2a-i] have been prepared by the cyclisation of 5-aryl-4-amino-3-mercapto-1,2,4-triazole by reaction with 2-chloro-3-formylquinoline in catalytic presence of p-toluene sulphonic acid. All the synthesized compounds have been characterized by elemental and spectral (IR, 1H- NMR and Mass) analysis. Furthermore, all compounds were evaluated for their antibacterial and antifungal activities against selected panel of pathogenic strains. Ampicillin trihydrate and fluconazole were used as standard drugs for antibacterial and antifungal activity, respectively. 3-(2-Chloro)phenyl-5H,13aH-quinolino(3,2-f)(1,2,4)triazolo(4,3-b)(1,2-diaza-4-sulpho)azepine [2h] was found, one of the most potent with lesser toxicity among the all prepared thiazepine derivatives.


2019 ◽  
Vol 31 (4) ◽  
pp. 528-533 ◽  
Author(s):  
Nagarjuna Reddy Desam ◽  
Abdul Jabbar Al-Rajab ◽  
Mukul Sharma ◽  
Mary Moses Mylabathula ◽  
Ramachandra Reddy Gowkanapalli ◽  
...  

2020 ◽  
Vol 1211 ◽  
pp. 128107 ◽  
Author(s):  
Akhilash Mohanan Pillai ◽  
Vishnu Sankar Sivasankarapillai ◽  
Abbas Rahdar ◽  
Jithu Joseph ◽  
Fardin Sadeghfar ◽  
...  

Author(s):  
Pallavi Kamble ◽  
Sailesh Wadher

 Objective: The objective of the present study was to synthesize a series of 3-hydroxychromone derivatives and to evaluate its in vitro antioxidant and antimicrobial activities.Methods: 3-hydroxy chromones were synthesized using an algar flynn oyamada method which includes oxidative cyclization of 2-hydroxy chalcones in basic solution by hydrogen peroxide. 2-hydroxy chalcones were synthesized by Claisen-Schmidt condensation of substituted 2-hydroxy acetophenones with substituted aromatic aldehydes using polyethylene glycol-400 as a recyclable solvent. The synthesized compounds were evaluated for in vitro antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl radical scavenging assay. In addition, these compounds were also screened for in vitro antibacterial and antifungal activity by agar cup method and Poison plate method, respectively.Results: The structures of the synthesized compounds were characterized by infrared, 1H nuclear magnetic resonance and mass spectroscopy. The antioxidant activity data revealed that all the synthesized derivatives exhibited good activity due to the presence of phenolic hydroxyl group, 4-oxo group and 2,3-double bond. Further, the activity increased with the introduction of a more phenolic hydroxyl group and adjacent methoxy group in the structure. The antimicrobial activity data showed that the compounds possess better antibacterial and antifungal activity which is attributed to the presence of phenolic hydroxyl group and 4-oxo group in the structure.Conclusions: The use of inexpensive, eco-friendly and readily available reagents, easy work-up and high purity of products makes the procedure a convenient and robust method for the synthesis of title compounds. The presence of phenolic hydroxyl group, 4-oxo group, and 2,3-double bond in the structure is responsible for their good antioxidant and antimicrobial activities.


2009 ◽  
Vol 7 (1) ◽  
pp. 73-80 ◽  
Author(s):  
Subhasish Saha ◽  
Dharumadurai Dhanasekaran ◽  
Sarvanan Chandraleka ◽  
Annamalai Panneerselvam

Cobalt complex with histidine ligand was synthesized and physico-chemically characterized by solubility testing, melting point, UV-spectra and FTIR. The synthesized metal complex was evaluated for in-vitro antibacterial and antifungal activity against the multidrug resistant pathogens, such as Pseudomonas aeruginosa, Vibrio cholerae, Salmonella typhi, E. coli, Klebsiella pneumonia, Staphylococcus aureus, Aspergillus niger, Aspergillus flavus and Candida albicans. The metal complex showed the significant antibacterial and antifungal activity comparison with commercial antibiotics. Further work can be extended through In-silico docking of this metal complex and bacterial, fungal genome which can be given a better idea about genome metal interaction in molecular level.


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