Synthesis and antimicrobial activities of novel quinoline derivatives carrying 1,2,4-triazole moiety

Eswaran, Sumesh; Adhikari, Airody Vasudeva; Shetty, N. Suchetha

doi:10.1016/j.ejmech.2009.06.031

Cited by 270 publications

(122 citation statements)

References 21 publications

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“…Triazole derivatives represent an interesting class of heterocyclic compounds; they possess many biological activities such as antimicrobial, anti-tubercular, anti-inflammatory and anticancer activities [16][17][18][19][20]. As an important type of nitrogen-containing aromatic heterocyclic compounds, 1,2,3-triazole was regarded as the bioisosteric replacement of itsbioisoster 1,2,4-triazole, amide, or even other nitrogen-containingaromatic heterocycles [21,22].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of water soluble chitosan derivatives with halogeno-1,2,3-triazole and their antifungal activity

Tan

Zhang

et al. 2016

International Journal of Biological Macromolecules

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a b s t r a c tChitosan is an abundant and renewable polysaccharide, which exhibits attractive bioactivities and natural properties. Improvement such as chemical modification of chitosan is often performed prior to further utilization. Three novel water soluble chitosan derivatives containing 1,2,3-triazole with or without halogen was designed and synthesized. Their antifungal activity against three kinds of phytopathogens was estimated by hyphal measurement in vitro. The inhibitory property and water solubility of the synthesized chitosan derivatives exhibited a remarkable improvement over chitosan. It is hypothesized that thiazolyl groups enable the synthesized chitosan to possess obviously better antifungal activity. Moreover, CTCTS and BTCTS, which have halogens at the periphery of polymers, inhibited the growth of tested phytopathogens more effectively with inhibitory indices of 81-93% at 1.0 mg/mL. The halogens could have a synergistic effect with triazole as they exhibited antifungal activity and electron-withdrawing capacity, which improve the antifungal activity of chitosan derivatives.

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Section: Introductionmentioning

confidence: 99%

Synthesis of water soluble chitosan derivatives with halogeno-1,2,3-triazole and their antifungal activity

Tan

Zhang

et al. 2016

International Journal of Biological Macromolecules

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“…The term reactive oxygen species encompasses a wide range of molecules. Free radicals are chemical species containing one or more unpaired electrons [25]. Therapeutic strategies that promote ROS accumulation and cell death have been explored based on the availability of drugs that interfere with scavenging.…”

Section: Intracellular Ros Levelmentioning

confidence: 99%

“…Erythrocytes were treated with PBS and SDS to obtain values corresponding to 0 and 100% of lysis, respectively [25]. The erythrocytes were incubated for 1 h with five different concentrations (0.1, 0.5, 1, 5 and 10 mM of compounds 6 g , 6 h and 6 k to measure hemolyticlysis.…”

Section: Hemolytic Assaymentioning

confidence: 99%

Design, Synthesis, Molecular Modelling and Biological Evaluation of Novel α-Naphtholhydroxamate Derivatives as Potential Anticancer Agents

Abdelrahim¹,

Mohan²,

Albarrati³

et al. 2016

Med chem (Los Angeles)

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Chemotherapy is one of the treatment options for cancer. A major problem in cancer chemotherapy is the lack of selective toxicity of many commonly used anti-cancer agents towards tumor tissue compared to normal tissue. Studies have shown that α-naphthol is selectively toxic to cultures of human tumor tissue compared to normal tissues in vitro. Hence, this study was conducted to synthesize a series of new hydroxamate derivatives containing α-naphthol nucleus by the reaction of naphthol acetic acid with amino acid methyl ester derivatives which were directly reacted with hydroxyl amine at room temperature. Structures of these compounds were confirmed by standard studies of IR, 1 H NMR, 13 CNMR, MS and elemental analysis. The cytotoxicity of the synthesized compounds were studied using the MTT assay in four human cancer cell lines, including HepG2, PC-3, HT-29 and MCF-7. Among the compounds, compound 6 g and 6 h exhibited a significant cytotoxicity against almost all the used cells including the normal cells . Further studies have shown that the cell death observed was closely associated with generation of reactive oxygen species (ROS). In this study, other naphthol derivatives have shown significant increase in the level of ROS in concentration dependent manner in treated cells. In conclusion, the study has shown that among the synthesized compounds, compounds 6 g , 6 k and 6 h hold the potential for further research. Furthermore, a molecular docking of the tested compounds was carried out to investigate their binding pattern with the prospective target, HDAC (PDB-code: 1T69).

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“…Discussion 1,2,4-Triazole derivatives have been extensively investigated because they possess awide spectrum of chemotherapeutic activities including anti-inflammatory [1,2], anticancer [3], antimicrobial [4][5][6], and antifungal [7]. In fact, some of their derivatives are active constituents of currently used drugs [6]. The title moleule consists of a1,2,4-triazole ring and aflexible chain (-C1-S1-C3-C4-)containing carboxy group (figure, top).…”

Section: Source Of Materialsmentioning

confidence: 99%

Crystal structure of 1H-1,2,4-triazole-3-mercaptoacetic acid, C4H5N3O2S

Wang¹,

Xin²,

Wang³

2010

Zeitschrift Für Kristallographie - New Crystal Structures

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Synthesis and antimicrobial activities of novel quinoline derivatives carrying 1,2,4-triazole moiety

Cited by 270 publications

References 21 publications

Synthesis of water soluble chitosan derivatives with halogeno-1,2,3-triazole and their antifungal activity

Synthesis of water soluble chitosan derivatives with halogeno-1,2,3-triazole and their antifungal activity

Design, Synthesis, Molecular Modelling and Biological Evaluation of Novel α-Naphtholhydroxamate Derivatives as Potential Anticancer Agents

Crystal structure of 1H-1,2,4-triazole-3-mercaptoacetic acid, C4H5N3O2S

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