scholarly journals Regioselective Synthesis of Dispiro Pyrrolizidines as Potent Antimicrobial Agents for Human Pathogens

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
N. Sirisha ◽  
R. Raghunathan

Synthesis of a series of novel dispiro pyrrolizidines has been accomplished by 1,3-dipolar cycloaddition reaction of azomethine ylide generated from secondary amino acids and diketones with bischalcones. These compounds were evaluated for their antibacterial activity. Most of the synthetic compounds exhibited good antibacterial activity against microorganisms.

SynOpen ◽  
2017 ◽  
Vol 01 (01) ◽  
pp. 0063-0067
Author(s):  
Sirisha Nallamala ◽  
Srikumar Mannem ◽  
Raghunathan Raghavachary

A variety of sugar-fused chromanono pyrrolidines/pyrrolizidines/thiolizidines have been synthesized by intermolecular 1,3-dipolar cycloaddition reaction of azomethine ylides (generated from glucose aldehyde and different secondary amino acids) with various 3-arylidene chroman-4-ones as dipolarophiles. The solvent effect on the 1,3-dipolar cycloaddition reaction is also studied.


2018 ◽  
Vol 16 (1) ◽  
pp. 3-10
Author(s):  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Pravin S. Wakte ◽  
Ajinkya P. Sarkate ◽  
Ashwini V. Izankar ◽  
...  

Background:A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.Objective:We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.Methods:A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.Results and Conclusion:From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.


2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
S. Boukhssas ◽  
Y. Aouine ◽  
H. Faraj ◽  
A. Alami ◽  
A. El Hallaoui ◽  
...  

The compound, diethyl 1-((4-methyl-2-phenyl-4,5-dihydrooxazol-4-yl)methyl)-1H-1,2,3-triazole-4,5-dicarboxylate 2, was synthesized in high yield, through 1,3-dipolar cycloaddition reaction of 4-(azidomethyl)-4-methyl-2-phenyl-4,5-dihydrooxazole and diethyl but-2-ynedioate in the absence of a solvent. The structure of the synthesized compound was established on the basis of NMR spectroscopy (1H, 13C), X-ray crystallography, and MS data. The prepared compound was also tested in vitro for its antibacterial activity against Gram-positive bacteria (Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli). The calculation of MBC/MIC ratio showed that this triazole derivative 2 had a bactericidal effect on the two strains tested.


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