Synthesis, Reactions and Antimicrobial Activity of Thieno[2,3-c]pyridazine Derivatives

2009 ◽  
Vol 2009 (10) ◽  
pp. 593-598 ◽  
Author(s):  
Fatma El Mariah

The reaction of N1-(un)substituted 4-aminosulfonamide with 6-chloropyridothienopyridazine (5) and 8-chloro-pyrimidothienopyridazine (14) gave 6-substituted aminopyridothienopyridazine (9) and 8-substituted amino-pyrimidothienopyridazine (16) respectively. All of the derivatives have been characterised by analytical and spectroscopic studies and also tested for their in vitro antibacterial and antifungal activity against a variety of microorganisms.

2013 ◽  
Vol 19 (1) ◽  
pp. 7-11
Author(s):  
Aleksandra Djordjevic ◽  
Jelena Lazarevic ◽  
Violeta Mitic ◽  
Radosav Palic ◽  
Gordana Stojanovic

The in vitro antimicrobial activity of Hypericum annulatum and Hypericum elegans essential oils was evaluated against a panel of standardized bacteria and fungi using broth microdilution assay. Both essential oils showed antimicrobial activity against all the tested microorganisms. Hypericum annulatum essential oil showed better antibacterial than antifungal activity, being more effective against Pseudomonas aeruginosa and Escherichia coli while H. elegans essential oil showed no significant difference between antibacterial and antifungal activity. Antimicrobial testing of ?-pinene, ?-pinene and ?-myrcene compounds was also performed. All the compounds were active against all the tested microorganisms, however, based on the MIC, MBC and MFC values, none of these compounds could be thought of as the main bearer of the oils? antimicrobial activity. This is the first report regarding the antimicrobial activity of the essential oils of the two Hypericum species.


2012 ◽  
Vol 77 (3) ◽  
pp. 279-286 ◽  
Author(s):  
Nirav Shah ◽  
Nimesh Shah ◽  
Manish Patel ◽  
Ranjan Patel

A simple and efficient method has been developed for the synthesis of some novel biquinoline derivatives bearing a thiazole moiety through a onepot three-component condensation of 2-chlro-3-formylquinolines, ethyl cyanoacetate and ?-enaminone using catalytic amount of piperidine in refluxing ethanol. These molecules were evaluated in vitro for their antibacterial and antifungal activity. Most of the compounds exhibited moderate antibacterial and antifungal activity against all the tested strains.


2009 ◽  
Vol 63 (5) ◽  
Author(s):  
Gülşah Kurt ◽  
Fatih Sevgi ◽  
Bedrettin Mercimek

AbstractIn this study, new benzoylthiourea derivatives, (E)-N-[(2-benzamidomethyleneamino)ethylcarbamothioyl]benzamide H3L′, N-(1-(3-benzoylthioureido)propan-2-ylcarbamothioyl)-benzamide H4L″, (E)-N-[4-(benzamidomethyleneamino)phenylcarbamothioyl]benzamide H3L‴, were synthesized. Structures of the compounds were identified by spectroscopic techniques. In addition, all synthesized compounds were evaluated for in vitro antibacterial and antifungal activity. Compound H3L‴ exhibited antibacterial activity.


Author(s):  
BHAGCHAND JAT ◽  
SWAPNA SANTRA ◽  
PRASANTA KUMAR SANTRA

Objectives: Synthesis, characterization, and evaluation of antimicrobial activity of novel pyrimidine derivatives containing O, N, and S in the ring. Methods: Pyrimidine derivatives were prepared in three steps. In the first step, chalcones containing -NO2 functional group were synthesized using Claisen-Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the second step, -NO2 group was reduced to -NH2 group. Resulting compounds containing NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,N-diisopropylethylamine to obtain pyrimidine derivatives.Antibacterial and antifungal activity of pyrimidine derivatives were studied in vitro. Results: Pyrimidine derivatives were synthesized and purified using flash column chromatography. Purity of synthesized pyrimidines was determined by high-performance liquid chromatography. Pyrimidines were characterized by elemental analysis, infrared, nuclear magnetic resonance, and mass spectral analysis. Analytical data of synthesized pyrimidines supported the proposed structures. Significant antibacterial and antifungal activity were observed in the synthesized pyrimidine derivatives. Conclusion: Antibacterial and antifungal activity of the newly synthesized pyrimidine derivatives will definitely inspire future researchers for the preparation of new analogs.


2015 ◽  
Vol 80 (7) ◽  
pp. 839-852 ◽  
Author(s):  
Nina Bozinovic ◽  
Irena Novakovic ◽  
Sladjana Kostic-Rajacic ◽  
Igor Opsenica ◽  
Bogdan Solaja

A series of new 5H-pyridobenzazepine and pyridobenzothiepine derivatives was synthesized by Pd-catalyzed formation of C-N and C-S bonds. All synthesized compounds were tested for their in vitro antimicrobial activity. The 5H-pyridobenzazepine derivatives showed better antibacterial and antifungal activity than corresponding 5H-dipyridoazepine analogs. Among the synthesized azepines, derivative 8 displayed potent activity against tested bacteria (MIC = 39-78 ?g/mL), while azepine 12 showed promising antifungal activity (MIC = 156-313 ?g/mL). The synthesized thiepine derivatives exhibited weak antibacterial activity, but showed pronounced antifungal activity.


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

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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