Synthesis, biological screening, in silico study and fingerprint applications of novel 1, 2, 4‐triazole derivatives

Khan, Ghouse; Sreenivasa, S.; Govindaiah, Shivaraja; Chandramohan, Vivek; P, Raghurama Shetty

doi:10.1002/jhet.3929

Cited by 15 publications

(5 citation statements)

References 49 publications

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“…According to our knowledge, there are only few reports in the literature on the anthelmintic activity of 1,2,4-triazole derivatives. In previous research on Indian worm Pheritima postuma activity of 1,2,4-triazole, the strongest anthelmintic activity showed derivatives possessing 2,4-dichlorophenyl [ 52 ], 4-chlorophenyl or 4-nitrophenyl moieties [ 53 ]. The diversity of substituents present in the most active compounds indicates various possibilities for the modification of potential nematicidal agents.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Anthelmintic and Anti-Inflammatory Activity of 1,2,4-Triazole Derivatives

et al. 2022

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Parasitic diseases, caused by intestinal helminths, remain a very serious problem in both human and veterinary medicine. While searching for new nematicides we examined a series of 1,2,4-triazole derivatives 9–22, obtained during reactions of N3-substituted amidrazones with itaconic anhydride. Two groups of compounds, 9–16 and 17–22, differed in the position of the double bond on the methacrylic acid moiety. The toxicity of derivatives 9–22 and the anti-inflammatory activity of 12 and 19–22 were studied on peripheral blood mononuclear cells (PBMC). Antiproliferative activity of compounds 12 and 19–22 was tested cytometrically in PBMC cultures stimulated by phytohemagglutinin. The influence of derivatives 12 and 19–22 on the TNF-α, IL-6, IL-10 and IFN-γ production was determined by ELISA in lipopolysaccharide-stimulated PBMC cultures. Anthelmintic activity of compounds 10–22 was studied in the Rhabditis sp. nematodes model. Most compounds (11–22) proved to be non-toxic to human PBMC. Derivatives 19–22 showed anti-inflammatory activity by inhibiting the proliferation of lymphocytes. Moreover, compounds 12 and 19–22 significantly reduced the production of TNF-α and derivatives 19–21 decreased the level of INF-γ. The strongest anti-inflammatory activity was observed for compound 21. Compounds 12 and 14 demonstrated anthelmintic activity higher than albendazole and may become promising candidates for anthelmintic drugs.

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Section: Discussionmentioning

confidence: 99%

Evaluation of Anthelmintic and Anti-Inflammatory Activity of 1,2,4-Triazole Derivatives

et al. 2022

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“…All triazole derivatives with N -alkylated groups were tested for fungicidal activity toward Candida albicans and Aspergillus flavus and anthelmintic activity against Pheretima posthuma , and the compound containing group CH 3 at the ortho position of the phenyl ring showed good inhibition with the inhibition zone 24.17 ± 0.32 and 15.02 ± 0.41 mm against A flavus and C albicans in comparison with a standard antifungal drug, Nystatin, while the antifungal activity of the other structures was lower ( Figure 38 ) [ 121 ].…”

Section: 124 Triazole Scaffold For the Development Of Antifungal Agentsmentioning

confidence: 99%

Novel 1, 2, 4-Triazoles as Antifungal Agents

Kazeminejad

Marzi

Shiroudi

et al. 2022

BioMed Research International

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The development of innovative antifungal agents is essential. Some fungicidal agents are no longer effective due to resistance development, various side effects, and high toxicity. Therefore, the synthesis and development of some new antifungal agents are necessary. 1,2,4-Triazole is one of the most essential pharmacophore systems between five-membered heterocycles. The structure-activity relationship (SAR) of this nitrogen-containing heterocyclic compound showed potential antifungal activity. The 1,2,4-triazole core is present as the nucleus in a variety of antifungal drug categories. The most potent and broad activity of triazoles have confirmed them as pharmacologically significant moieties. The goal of this review is to highlight recent developments in the synthesis and SAR study of 1,2,4-triazole as a potential fungicidal compound. In this study, we provide the results of a biological activity evaluation using various structures and figures. Literature investigation showed that 1, 2, 4-triazole derivatives reveal the extensive span of antifungal activity. This review will assist researchers in the development of new potential antifungal drug candidates with high effectiveness and selectivity.

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“…Many investigations have been conducted with triazole, which are important for the development of new medicines [4]. Triazole derivative's unusually structure and electron-rich system allow them to interact easily with a variety of receptors, resulting in a wide range of biological activities [5]. Antibacterial, antifungal and anticancer properties are only a few of the interesting pharmacological properties of adamantane derivatives [6][7][8].…”

Section: Introductionmentioning

confidence: 99%

Adsorption Behavior of an Adamantane Derivative on Metal Clusters – DFT Simulation Studies

Al‐Otaibi¹,

Mary²,

Mary³

2021

Preprint

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Investigation of the adsorption properties of 3-(adamantan-1-yl)-4-phenyl-1-[(4-phenylpiperazin-yl)methyl]-1H-1,2,4-triazole-5(4H)-thione (APT) with metal clusters (mC: Ag, Au and Cu) are reported using DFT method. APT is found to form stable cluster with transition metal clusters of copper, silver and gold. The drug-cluster complexation energy is slightly more for the gold nanocluster-drug complex. Dipole moment of the drug-gold cluster is found to be higher than that of the other systems. SERS studies demonstrate improved Raman signals for multiple wavenumbers of all APT-metal cluster complexes. Different spectroscopic, chemical and electronic properties are also investigated.

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Synthesis, biological screening, in silico study and fingerprint applications of novel 1, 2, 4‐triazole derivatives

Cited by 15 publications

References 49 publications

Evaluation of Anthelmintic and Anti-Inflammatory Activity of 1,2,4-Triazole Derivatives

Evaluation of Anthelmintic and Anti-Inflammatory Activity of 1,2,4-Triazole Derivatives

Novel 1, 2, 4-Triazoles as Antifungal Agents

Adsorption Behavior of an Adamantane Derivative on Metal Clusters – DFT Simulation Studies

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