Synthesis, structural elucidation and bioevaluation of 4-amino-1,2,4-triazole-3-thione’s Schiff base derivatives

2015 ◽  
Vol 39 (2) ◽  
pp. 161-171 ◽  
Author(s):  
Muhammad Rafiq ◽  
Muhammad Saleem ◽  
Muhammad Hanif ◽  
Sung Kwon Kang ◽  
Sung-Yum Seo ◽  
...  
Keyword(s):  
Schiff Base ◽  
Structural Elucidation ◽  
Schiff Base Derivatives

Efficacy of Novel Schiff base Derivatives as Antifungal Compounds in Combination with Approved Drugs Against Candida Albicans

2019 ◽  
Vol 15 (6) ◽  
pp. 648-658 ◽  
Author(s):  
Manzoor Ahmad Malik ◽  
Shabir Ahmad Lone ◽  
Parveez Gull ◽  
Ovas Ahmad Dar ◽  
Mohmmad Younus Wani ◽  
...  
Keyword(s):  
Schiff Base ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Fungal Infections ◽  
Total Sterol ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Ergosterol Biosynthesis ◽  
Dependent Manner ◽  
Schiff Base Derivatives

Background: The increasing incidence of fungal infections, especially caused by Candida albicans, and their increasing drug resistance has drastically increased in recent years. Therefore, not only new drugs but also alternative treatment strategies are promptly required. Methods: We previously reported on the synergistic interaction of some azole and non-azole compounds with fluconazole for combination antifungal therapy. In this study, we synthesized some non-azole Schiff-base derivatives and evaluated their antifungal activity profile alone and in combination with the most commonly used antifungal drugs- fluconazole (FLC) and amphotericin B (AmB) against four drug susceptible, three FLC resistant and three AmB resistant clinically isolated Candida albicans strains. To further analyze the mechanism of antifungal action of these compounds, we quantified total sterol contents in FLC-susceptible and resistant C. albicans isolates. Results: A pyrimidine ring-containing derivative SB5 showed the most potent antifungal activity against all the tested strains. After combining these compounds with FLC and AmB, 76% combinations were either synergistic or additive while as the rest of the combinations were indifferent. Interestingly, none of the combinations was antagonistic, either with FLC or AmB. Results interpreted from fractional inhibitory concentration index (FICI) and isobolograms revealed 4-10-fold reduction in MIC values for synergistic combinations. These compounds also inhibit ergosterol biosynthesis in a concentration-dependent manner, supported by the results from docking studies. Conclusion: The results of the studies conducted advocate the potential of these compounds as new antifungal drugs. However, further studies are required to understand the other mechanisms and in vivo efficacy and toxicity of these compounds.

scholarly journals Synthesis and Evaluation of Schiff Bases of 4-Amino-5-(chlorine substituted phenyl)-4H-1,2,4-triazole-3-thione as Antimicrobial Agents

2020 ◽  
Vol 41 (1) ◽  
pp. 26-35
Author(s):  
Kishor Devkota ◽  
Govinda Pathak ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Triazole Ring ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Spectral Techniques ◽  
Schiff Base Derivatives ◽  
Bacteria And Fungi ◽  
Different Strains

Triazole ring system has attracted a continuously growing interest of synthetic organic chemists and those dealing with the medicinal compounds due to its versatile potential to interact with biological systems. Schiff bases are also considered as one of the most biologically active compounds.  The aim of the present study was to synthesize new Schiff bases bearing triazole nucleus and to assess their antimicrobial activities. Four new Schiff base derivatives of 1,2,4-triazole-3-thione were synthesized by combining two different pharmacophores viz. triazole nucleus and Schiff base moiety and were characterized by spectral techniques (UV, FT-IR, and NMR). The Schiff bases were evaluated for antibacterial (Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae) and antifungal (Candida albicans) activities. The synthesized compounds exhibited good to moderate activities against different strains of bacteria and fungi tested.

Synthesis, in vitro and in vivo antitumor activity of symmetrical bis-Schiff base derivatives of isatin

2014 ◽  
Vol 74 ◽  
pp. 742-750 ◽  
Author(s):  
Chengyuan Liang ◽  
Juan Xia ◽  
Dong Lei ◽  
Xiang Li ◽  
Qizheng Yao ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Schiff Base Derivatives ◽  
In Vivo Antitumor Activity ◽  
Derivatives Of

Terminal Organylchalcogenoethyl- and -propylamines and Their Schiff Base Derivatives

Synthesis ◽  
2005 ◽  
pp. 1641-1648 ◽  
Author(s):  
Svetlana V. Amosova ◽  
Natalia A. Makhaeva ◽  
Alexander V. Martynov ◽  
Vladimir A. Potapov ◽  
Barry R. Steele ◽  
...  
Keyword(s):  
Schiff Base ◽  
Schiff Base Derivatives

Microcalorimetric Study on the Inhibition ofEscherichia coliby Some Novel Pyridine Amide Schiff Base Derivatives

2008 ◽  
Vol 26 (9) ◽  
pp. 1573-1578 ◽  
Author(s):  
Chao-Hong LI ◽  
Li-Xia ZHANG ◽  
Li-Hua CAI ◽  
Yi LIU ◽  
Pei-Zhi HU
Keyword(s):  
Schiff Base ◽  
Schiff Base Derivatives

Biological Evaluation and Synthesis of Thiazole Schiff Base Derivatives

Heterocycles ◽  
2021 ◽  
Vol 102 (7) ◽  
pp. 1337
Author(s):  
Jinbing Liu ◽  
Wei Zhou ◽  
Fengyan Wu
Keyword(s):  
Schiff Base ◽  
Biological Evaluation ◽  
Schiff Base Derivatives

SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF SOME SCHIFF BASES OF 1, 3, 4-OXADIAZOLE

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 12-17
Author(s):  
Manpreet Kaur ◽  
S. Singh ◽  
Keyword(s):  
Schiff Base ◽  
Growth Inhibition ◽  
Anticancer Activity ◽  
Maximum Growth ◽  
Schiff Base Derivatives ◽  
Control Growth ◽  
Anti Cancer ◽  
Oxadiazole Derivatives ◽  
Cancer Activity ◽  
Mcf 7

A new series of 2,5-disubstituted-1,3,4-oxadiazole derivatives has been synthesized with the help of different aromatic benzaldehydes and final compounds were characterized by FTIR and 1H NMR. 2,5- disubstituted-1,3,4-oxadiazole derivatives were synthesized by the reaction of Schiff base derivatives with 2,5-disubstituted-1,3,4-oxadiazoles. All the synthesized compounds were screened for their anticancer activity. These compounds were evaluated for their anticancer activity against various cancer cell lines. Five of the compounds possessed good to moderate anti-cancer activity. Three of the synthesized compounds i.e. 6a, 6f and 6g were found to possess maximum growth inhibition. The order for the % control growth inhibition of MCF-7 was found to be 6a>6f>6g>5b>6h, as shown in Table II-VI.

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