<scp>Synthesis and biological evaluation of novel 2‐arylquinoline‐3‐fused thiazolo</scp>[2,3‐c]1,2,<scp>4‐triazole heterocycles as potential antiproliferative and antimicrobial agents</scp>

Dhanavath, Ramulu; Dharavath, Ravinder; Kothula, Devender; Bitla, Sampath; Yaku, Gugulothu; Birdaraju, Saritha; Puchakayala, Muralidhar Reddy; Raju, Archana

doi:10.1002/jhet.4460

Cited by 4 publications

(6 citation statements)

References 40 publications

(45 reference statements)

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“…This is evi-denced by the use of drugs Itraconazole, Fluconazole in the world medical practice. The works of scientists [11][12][13][14][15][16][17][18][19][20] confirm this. Systematizing the literature, we can conclude that the substituents adamantane, 5-amino-2-hydroxybenzoate, 4-fluoro-2-phenoxyphenyl, 2-bromophenyl and hydroxybenzylidene fragment in the 5 position of the heterocyclic system of 1,2,4-triazole lead to an increase in antifungal action.…”

Section: Antifungal Activity Of 124-triazole Derivativesmentioning

confidence: 74%

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Prospects for the search for new biologically active compounds among the derivatives of the heterocyclic system of 1,2,4-triazole.

et al. 2022

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The authors are not native speakers of Turkish The purpose of this literature review was to systematize data from studies of the biological activity of 1,2,4-triazole derivatives with substituents in positions 4 and 5. The authors set the task of forming an idea of current directions in the selection of substitutions for 1,2,4-triazole based on research. As a result of the study, 75 literature sources were analyzed. This made it possible to form a further vector in terms of searching for biologically active structures among 1,2,4-triazole derivatives. The review develops a modern approach to the search for biologically active substances among 1,2,4-triazole derivatives. Systematized data on the nature of substituents in the core of 1,2,4-triazole, which affect a specific type of activity. The search material was selected over the past decade with the highest number of citations at the time of literature analysis.

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Section: Antifungal Activity Of 124-triazole Derivativesmentioning

confidence: 74%

“…1). The results considered in [11][12][13][14][15][16][17][18][19] indicate inhibition P. cubensis, A. niger, S. fuligenea, F. oxysporum, X. Axonopodis, C. cassiicola and other strains of pathogenic fungi.…”

Section: Antifungal Activity Of 124-triazole Derivativesmentioning

confidence: 99%

Prospects for the search for new biologically active compounds among the derivatives of the heterocyclic system of 1,2,4-triazole.

et al. 2022

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“…These results align with previously published studies that have reported on the antibacterial and antifungal properties of similar compounds. 39 Based on the obtained results, it is evident that the synthesized triazole derivatives have the potential to serve as valuable agents for the design and development of novel therapeutic drugs to combat bacterial resistance.…”

mentioning

confidence: 92%

Synthesis, Biological Evaluation and Molecular Docking Studies of Novel Series of Bis-1,2,4-Triazoles as Thymidine Phosphorylase Inhibitor

Korol,

Holovko-Kamoshenkova,

Slivka

et al. 2023

AABC

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Heterocyclic compounds have diverse biological activities and potential in drug development. This study aims to synthesize novel compounds with two 1,2,4-triazole cores and evaluate their biological properties, particularly their inhibitory activity against thymidine phosphorylase (TP), an enzyme involved in various physiological processes. Methods: The compounds were synthesized by reacting 5,5'-butane-bis-1,2,4-triazole derivatives with prenyl bromide. Characterization involved various techniques, including spectroscopy and elemental analysis. Antimicrobial potential was evaluated against bacteria and fungi, with comparative antibiotics as references. Inhibitory activity against TP was assessed, and molecular docking studies were conducted. Results: Six compounds were successfully synthesized and their structures confirmed. The synthesized triazole derivatives exhibited high biological activity, with compounds 2 and 6 showing the most promising TP inhibition. Molecular docking studies revealed interactions between compound 2 and TP, involving nine amino acids. Discussion: The synthesis of novel compounds with two 1,2,4-triazole cores contributes significantly to bis-triazole research. These compounds have potential as anti-tumor agents due to their inhibitory activity against TP, a crucial enzyme in tumor growth and metastasis. Comparative evaluation against antibiotics highlights their potency. Docking results provide insights into their interactions with TP, supporting their potential as potent TP inhibitors. Further research should focus on evaluating their efficacy in biological models, understanding their mechanisms of action, and optimizing their activities. Conclusion:The synthesized compounds with two 1,2,4-triazole cores exhibit significant biological activity, including strong TP inhibition and broad-spectrum antimicrobial effects. These findings emphasize their potential as anti-tumor agents and the need for further exploration and optimization. Future research should focus on evaluating their efficacy in biological models, understanding their mechanisms of action, and developing more potent bis-triazole derivatives for drug discovery efforts. The combined results from assays and docking studies support the therapeutic potential of these compounds as anti-tumor agents.

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“…The 1,2,4-triazoles derivatives have been found to possess wide spectrum of biological activities [30][31][32][33]. Numerous triazole-based drugs has been developed as antibacterial [34], antifungal [35], anti-malarial [36], anticancer [37], antidiabetic [38].…”

Section: Introductionmentioning

confidence: 99%

Syntheses and Antioxidant Activity of 1-Isonicotinoyl-4-phenylthiosemicarbazide and Crystal Structures of N-Phenyl-5-(pyridin-4-yl)-1,3,4-oxadiazol-2-amine Hydrochloride and 4-Phenyl-3-(pyridin-4-yl)-1H-1,2,4-triazole-5(4H)-thione derived from 1 Isonicotinoyl-4-phenylthiosemicarbazide

Faye

Mbow

Gaye

et al. 2022

EJCS

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The title compound C13H12N4OS (I) is synthetized from isonicotinic hydrazide and isothiocynate. Compounds C13H11N4OCl (II) and C13H10N4S (III) where obtained upon reaction of (I) with Fe(II) or Mn(II) salts. Compound (II) is heterocyclic 1,3,4-oxadiazole while compound (III) is heterocyclic 1,2,4-triazole. The 1,3,4-oxadiazol derivative is almost planar with dihedral angle of 2.66 (8) and 5.14 (8)° between 1,3,4-oxadiazole ring and phenyl and pyridinium rings respectively; the dihedral angle between the phenyl and pyridinium rings is 3.92 (8)°. The 1,2,4-triazole derivative is non-planar. The phenyl and pyridyl rings form dihedral angles of 58.35 (5) and 58.33 (5)°, respectively, with the 1,2,4-triazole ring; the dihedral angle between the phenyl and pyridyl rings is 36.85 (4)°. In the compound (II) intramolecular hydrogen bonds of type N—H···Cl, C—H···N and C—H···Cl resulting in S(6) ring stabilize the structure. Intermolecular hydrogen bonds of type N—H···N, C—H···N, C—4···Cl link the molecule thus forming a three-dimensional network. In the structure of compound (III), intermolecular hydrogen bonds of type N—H···N, C—H···N, C—H···S1,link the monomer in a three-dimensional network.

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Synthesis and biological evaluation of novel 2‐arylquinoline‐3‐fused thiazolo[2,3‐c]1,2,4‐triazole heterocycles as potential antiproliferative and antimicrobial agents

Cited by 4 publications

References 40 publications

Prospects for the search for new biologically active compounds among the derivatives of the heterocyclic system of 1,2,4-triazole.

Prospects for the search for new biologically active compounds among the derivatives of the heterocyclic system of 1,2,4-triazole.

Synthesis, Biological Evaluation and Molecular Docking Studies of Novel Series of Bis-1,2,4-Triazoles as Thymidine Phosphorylase Inhibitor

Syntheses and Antioxidant Activity of 1-Isonicotinoyl-4-phenylthiosemicarbazide and Crystal Structures of N-Phenyl-5-(pyridin-4-yl)-1,3,4-oxadiazol-2-amine Hydrochloride and 4-Phenyl-3-(pyridin-4-yl)-1H-1,2,4-triazole-5(4H)-thione derived from 1 Isonicotinoyl-4-phenylthiosemicarbazide

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