Synthesis and Antifungal Activity Evaluation of New 1,2,4-Triazole Derivatives Bearing Salicylidene Hydrazide Moiety

2015 ◽  
Vol 13 (2) ◽  
pp. 178-184
Author(s):  
Seref Demirayak ◽  
Ismail Kayagil ◽  
Leyla Yurttas ◽  
Sevda Er
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.


2020 ◽  
Vol 18 ◽  
Author(s):  
Niranjan Kaushik ◽  
Nitin Kumar ◽  
Anoop Kumar ◽  
Vikas Sharma

Background: Fungal infections are opportunistic infections that become a serious problem to human health. Objective: Considering the antifungal potential of triazole nucleus, the study was carried out with the objective to synthesize some novel triazole derivatives with antifungal potential. Method: 1,2,4-triazole derivatives were synthesized via a two step reaction (reported earlier). The first step involves reaction of substituted benzoic acid with thiocarbohydrazide to form 4-amino-3-(substituted phenyl)-5-mercapto-1, 2, 4-triazole derivatives (1a-1k) while in second step, synthesized compounds (1a-1k) were then subsequently treated with substituted acetophenone to yield substituted (4-methoxyphenyl-7H-[1, 2, 4] triazolo [3, 4-b][1,3,4] thiadiazine derivatives (2a-2k). All synthesized compounds were characterized by IR, 1H NMR, and Mass spectral data analysis and were screened for their antifungal properties against different fungal strains i.e. Candida tropicalis (ATCC-13803, ATCC-20913), Candida albicans (ATCC-60193), Candida inconspicua (ATCC-16783) and Candida glabrata (ATCC-90030, ATCC-2001). Results: Compound 2d displayed better percentage inhibition (26.29%, 24.81%) than fluconazole (24.44%, 22.96%) against ATCC-16783, ATCC-2001 fungal strains respectively at 100µg/ml. Compound 2f also displayed better percentage inhibition (28.51%) against ATCC-90030 as compared to fluconazone (27.4%) at 200 µg/ml. Similarly, compounds 2e and 2j also exhibited better antifungal properties than fluconazole at 200µg/ml. Compound 2e was found most potent against ATCC13803 (30.37%) and ATCC-90030 (30.37%) fungal strains as compared to fluconazole (28.14%, 27.4%) at 200 µg/ml respectively whereas compound 2j exhibited better antifungal activity (28.51%) against ATCC-60193 than fluconazole (27.7%) at 200 µg/ml. Conclusion: The results were in accordance with our assertions for triazole derivatives, as all compounds displayed moderate to good antifungal activity.


2017 ◽  
Vol 55 (1) ◽  
pp. 258-264 ◽  
Author(s):  
Salama A. Ouf ◽  
Sobhi M. Gomha ◽  
Mohamed M. Ewies ◽  
Ihab A. A. Sharawy

2019 ◽  
Vol 70 (10) ◽  
pp. 3522-3526
Author(s):  
Smaranda Oniga ◽  
Catalin Araniciu ◽  
Gabriel Marc ◽  
Livia Uncu ◽  
Mariana Palage ◽  
...  

Considering the well-established antifungal activity of azole compounds, a new series of thiazolyl-methylen-1,3,4-oxadiazolines derivatives were designed and synthesized as lanosterol-demethylase inhibitors. The final compounds were screened for antifungal activity against the Candida albicans ATCC 90028 strain. Molecular docking studies were performed to investigate the interaction modes between the compounds and the active site of lanosterol 14a-demethylase, which is a target enzyme for anticandidal azoles. Theoretical ADME predictions were also calculated for the final compounds 5a-h.


Author(s):  
Anuja Patil ◽  
Mohite Shriniwas

Azole exhibits wide range of pharmacological properties. there is limited number of drugs are available to treat microbial infection that too have serious toxic effects the existing drugs has been suffering from the development of resistance and thus newer drugs are required with better activity profile. In this paper synthesis of 1,3,4- oxadiazole derivative with precursor salicylic acid and perform an antifungal activity.


2019 ◽  
Vol 57 (3) ◽  
pp. 1379-1386
Author(s):  
Wen‐Neng Wu ◽  
Yang‐Ming Jiang ◽  
Qiang Fei ◽  
Hai‐Tang Du ◽  
Mao‐Fa Yang

2011 ◽  
Vol 83 (3) ◽  
pp. 715-722 ◽  
Author(s):  
Yury Morzherin ◽  
Polina E. Prokhorova ◽  
Dmitry A. Musikhin ◽  
Tatiana V. Glukhareva ◽  
Zhijin Fan

A series of novel 5-(2-hydroxypropyl)amino-1,2,3-thiadiazole and 5-(2-hydroxy-propyl)sulfanyl-1,2,3-triazole derivatives were designed and synthesized as candidate fungicides. The new compounds were identified by NMR and IR spectroscopy, mass spectrometry, and elemental analysis. Their antifungal activities were evaluated.


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