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1

Fizer, O. I., M. M. Fizer, A. O. Kryvoviaz, and M. V. Slivka. "INVESTIGATION OF THE INFLUENCE OF THE SUBSTITUTE IN THE THIRD POSITION ON THE ELECTRONIC STRUCTURE OF 1,3-THIAZOLO[2,3-c][1,2,4]TRIAZOLE." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 46, no. 2 (2022): 55–62. http://dx.doi.org/10.24144/2414-0260.2021.2.55-62.

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Condensed 1,2,4-triazole derivatives exhibit a wide range of biological activity. In particular, triazolam, alprazolam and estazolam, which contain [1,2,4]triazolo[4,3-a][1,4]benzodiazepine system, are used as tranquilizers. Brotizolam is another tranquilizer, a derivative of thieno[3,2-f][1,2,4]triazolo [4,3-a][1,4]diazepine. The oral hypoglycemic drug sitagliptin contains the [1,2,4]triazolo[4,3-a]pyrazine system. In addition, pesticides such as flumetsulam, metosulam, cloransulam, diclosulam, florasulam, are derivatives of [1,2,4]triazolo[1,5-a]pyrimidine, [1,2,4]triazolo[1,5-c]pyrimidine a
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Hryhorka, H. V., М. М. Fizer, О. І. Fizer, A. O. Kryvoviaz, and M. V. Slivka. "SYNTHESIS AND CHEMICAL PROPERTIES OF 2-HEPTADECYL-[1,3]THIAZOLO[3,2-b][1,2,4]TRIAZOL-7-IUM CATION." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 48, no. 2 (2023): 67–72. http://dx.doi.org/10.24144/2414-0260.2022.2.67-72.

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Functional and condensed derivatives of 1,2,4-triazoles are mostly used as biologically active compounds, and modern studies increasingly report their successful use as surfactants, stabilizers for the formation of nanoparticles, components of hybrid perovskites, which are promising materials for opto-electronics.
 Synthesis of new [1,3]thiazolo[3,2-b][1,2,4]triazol-7-ium salts containing a long-chain heptadecyl substituent was proposed within our research. The production of the starting compounds (2-heptadecyl-4-methyl-1,2,4-triazole-3-thione and methallyl thioether of 2-heptadecyl-3-mer
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3

GAMAL, A. AHMED. "Studies on 3-Amino-I ,2,4-triazole." Journal of Indian Chemical Society Vol. 74, Aug 1997 (1997): 624–25. https://doi.org/10.5281/zenodo.5891468.

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Department of Chemistry , Faculty of Science, Zagazig University, Zagazig, Egypt <em>Manuscript received 16 October 1995, revised 18 June 1996, accepted 24 July 1996</em> 1,2,4-Triazolo[2,3-a]-1,3,5-triazine-4-aryl-4-thiones (3a,b) and 5-(aroylamino)-1,2,4-triazoles (5a,b) have been synthesised by the reaction of 3-amino-1,2,4-triazole (1) with aroyl isothiocyanates. Also, 1 when reacted with cinnamonitrile derivatives yields the trlazolopyrimldine derivatives (6, 7a,b and 8). Treatment of 8 with carbon disulphide and formaide gives 9 and 10 respectively. Some of the compounds possess antimicr
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4

Syrota, Natalia O., Sergiy V. Kemskiy, Lesya M. Saliyeva, and Mykhailo V. Vovk. "1,2,3-Triazole-4(5)-amines – Convenient Synthetic Blocks for the Construction of Triazolo-Annulated Heterocycles." Journal of Organic and Pharmaceutical Chemistry 20, no. 2 (2022): 27–51. http://dx.doi.org/10.24959/ophcj.22.258512.

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Aim. To analyze and summarize the synthetic potential of 1,2,3-triazole-4(5)-amines as efficient building blocks in the synthesis of triazolo-annulated pyridine, azine and azepine systems.Results and discussion. Original literature sources revealing the synthetic potential of 4(5)-amino functionalized 1,2,3-triazoles as convenient and available building blocks for the preparation of triazolo-annulated pyridines, azines and azepines were analyzed and systematized. Condensation of 1,2,3-triazole-4(5)-amines with methylene active compounds was shown to be a powerful tool for the synthesis of vers
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5

Frolova, Yu S., A. H. Kaplaushenko, T. V. Ihnatova, and T. M. Kaplaushenko. "Synthesis methods of 1,2,4-triazole-3-thiones: review." Current issues in pharmacy and medicine: science and practice 17, no. 2 (2024): 187–96. http://dx.doi.org/10.14739/2409-2932.2024.2.302616.

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1,2,4-Triazole-containing compounds are unique heterocyclic compounds present in an array of pharmaceuticals and biologically important compounds used in drug-discovery studies against cancer cells, microbes, and various types of diseases in the human body. The aim of the study was to analyze in detail and combine the available literature materials to study the reactions associated with the formation of different classes of derivatives of 1,2,4-triazole-3-thione and to study their physical-chemical properties. Various innovative methods have been proposed and explored for synthesizing differen
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6

Zeng, Qun, Yanyang Qu, Jinshan Li, and Hui Huang. "Theoretical studies on the derivatives of tris([1,2,4]triazolo)[4,3-a:4′,3′-c:4′′,3′′-e][1,3,5]triazine as high energetic compounds." RSC Advances 6, no. 7 (2016): 5419–27. http://dx.doi.org/10.1039/c5ra22524h.

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7

Karpun, Yevhen, and Nataliia Polishchuk. "Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol." ScienceRise: Pharmaceutical Science, no. 3(31) (June 30, 2021): 64–69. http://dx.doi.org/10.15587/2519-4852.2021.235976.

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The aim of the work. 1,2,4-triazole derivatives possess a wide range of pharmacological activity, so they are used for the development of drugs and active pharmaceutical ingredients. Due to the reactivity of 1,2,4-triazoles there are many options for their further structural modification on different reaction centers. Therefore, the aim of the work was to obtain new S-substituted derivatives of 1,2,4-triazole-3-thiols, study physicochemical parameters of the substances synthesized, evaluate the antimicrobial activity of new S-derivatives of the 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)t
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8

Md, Akram* Abdul Sayeed Mohd Waseem Akram MD Ather Ali Soherwardi. "STUDIES ON THE SYNTHESIS OF SOME NEW 1,2,4- TRIAZOLES DERIVATIVES AND EVALUATION FOR THEIR ANTI-FUNGAL ACTIVITY PROFILES." Indo American Journal of Pharmaceutical Sciences 04, no. 08 (2017): 2234–48. https://doi.org/10.5281/zenodo.839545.

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The synthesis of new heterocyclic compounds has always drawn the attention of medicinal chemist over the years mainly because they possess diverse biological properties. The literature survey on 1,2,4-triazoles revealed that they are endowed with wide variety of biological activities .During the present investigation a series of new 1,2,4-triazole derivatives N-(3-(2-(3- hydrazinyl-3-oxoalkanoyl)hydrazinyl)-5-(phenoxymethyl)-4H-1,2,4-triazol-4-yl)isonicotinamide(6a- 6e)were synthesized by reacting withN-(5-mercapto-3-(phenoxymethyl)-4H-1,2,4-triazol-4- yl)isonicotinamide (5) and aliphatic dica
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9

Gotsulya, A. S., A. I. Panasenko, E. G. Knysh, and A. O. Pryimenko. "UV-spectrophotometric study of the 7-((3-thio-4-R-1,2,4-triazole-3-yl)methyl)-theophyllines." Farmatsevtychnyi zhurnal, no. 4 (September 4, 2018): 65–70. http://dx.doi.org/10.32352/0367-3057.4.15.03.

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Chemistry of the 1,2,4-triazole derivatives recently attracts the attention of many scientists, mainly due to the presence of the number of the valuable pharmacological properties. In modern medical practice, there are many examples of successful heterocyclic systems derivatives usage. First of all, it is a group of drugs with antifungal activity (fluconazole, itraconazole, voriconazole, pozakonazol), antidepressant activity (alprazolam, triazolam), anticancer activity (anastrozole, letrozole). But despite the great practical importance of works in this area, the structure of 1,2,4-triazoles-3
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10

Abhiman, S. Jadhav* Vinayak S. Marulkar V. Y. Lokhande Rupesh R. Shinde Pratik S. Dharmasale. "A Review On: Antibacterial And Antifungal Activity Of 1,2,3-Triazoles And 1,2,4-Triazole Derivatives." International Journal in Pharmaceutical Sciences 2, no. 8 (2024): 2860–87. https://doi.org/10.5281/zenodo.13292951.

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<strong>1,2,3-Triazoles:</strong> Triazoles are renowned scaffolds that are simple to conjugate with additional heterocyclic groups. These compounds exhibit a variety of pharmacological effects, including antibacterial and anticancer activities. Researchers have targeted these triazole-conjugated structural motifs as common pharmacological targets. Additionally, a study synthesized and evaluated the antibacterial properties of 1,2,3-triazole derivatives. Some of these compounds demonstrated good antibacterial activity, making them potential candidates for further investigation. <strong>1,2,4-T
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11

Khomenko, Dmytro, Tetyana Shokol, Roman Doroshchuk, Ilona Raspertova, Rostyslav Lampeka, and Yulian Volovenko. "Strategies for the Synthesis of [1,2,4]Triazolo[1,5-a]pyridine-8-carbonitriles." Chemistry & Chemical Technology 17, no. 2 (2023): 294–303. http://dx.doi.org/10.23939/chcht17.02.294.

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Conjugated heterocyclic compounds with a 1,2,4-triazole core are of scientific interest due to their wide application in both synthetic and medicinal chemistry. In this review, we comprehensively summarize the synthetic methods for [1,2,4]triazolo[1,5-a]pyridine-8-carbonitriles. The methods are classified as follows: convertion of 8-substituted [1,2,4]triazolo[1,5-a]pyridines; synthesis based on functionalized pyridines, containing a nitrile group; synthesis based on heterocyclization of 2-(1,2,4-triazol-5-yl)acetonitriles, including cyclocondensation of 2-(1,2,4-triazol-5-yl)acetonitriles wit
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12

Yevhen, Karpun, and Polishchuk Nataliia. "Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol." ScienceRise: Pharmaceutical Science, no. 3(31) (June 30, 2021): 64–69. https://doi.org/10.15587/2519-4852.2021.235976.

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<strong>The aim of the work.</strong>&nbsp;1,2,4-triazole derivatives possess a wide range of pharmacological activity, so they are used for the development of drugs and active pharmaceutical ingredients. Due to the reactivity of 1,2,4-triazoles there are many options for their further structural modification on different reaction centers. Therefore, the aim of the work was to obtain new S-substituted derivatives of 1,2,4-triazole-3-thiols, study physicochemical parameters of the substances synthesized, evaluate the antimicrobial activity of new S-derivatives of the 4-R1-5-((3-(pyridin-4-yl)-1
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13

Franco, Daiana Portella, Lucas Caruso, Nathalia Fonseca Nadur, Thiago Moreira Pereira, Renata Barbosa Lacerda, and Arthur Eugen Kümmerle. "Recent Advances in Microwave-Assisted Synthesis and Functionalization of 1,2,3- and 1,2,4-triazoles." Current Organic Chemistry 25, no. 23 (2021): 2815–39. http://dx.doi.org/10.2174/1385272825666211011111408.

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Triazoles are five-membered aromatic heterocyclics, which exhibit two isosteric forms (1,2,3-triazoles and 1,2,4-triazoles), as well as multiple applications in medicinal, agricultural, supramolecular, and materials sciences. Famous examples of triazoles include drugs, such as fluconazole, ribavirin, cefatrizine, and tazobactam, as well as herbicides, such as cafenstrole and metosulam. This review aims to present the recent major examples of the application of microwave-assisted organic synthesis (MAOS) to the syntheses and endfunctionalizations of 1,4- and 1,5-disubstituted 1,2,3-triazoles, 1
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Nurhan G mr k o lu, Nurhan G. mr k. o. lu, and Muhammad Imran and Inam Iqbal Muhammad Imran and Inam Iqbal. "Synthesıs and Characterızatıon of New Trıazole and Coumarın-Derived Heterocyclıc Compounds Part I." Journal of the chemical society of pakistan 41, no. 6 (2019): 1097. http://dx.doi.org/10.52568/000830/jcsp/41.06.2019.

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Synthesis of ethyl ester of acetic acid containing 5-oxo-[1,2,4] triazole ring (2) was achieved by the condensation of 3-substituted-4-amino-1H-1,2,4-triazol-5(4H)-one (1) with ethyl bromoacetate in basic medium. Compound 2, was then further reacted with hydrazine hydrate to form acid hydrazide, which is 2-(4-amino-3-substituted-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)acetohydrazide (3). Compound 3 was later treated with three different diverse coumarin aldehydes (6, 12, 18) resulted in the formation of arylidene hydrazides as cis–trans conformers (7, 8, 13, 14, 19, 20). In conclusion, we synt
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15

Sonawane, R., and M. A. Sagare. "Design, Synthesis and Evaluation of Some Substituted Triazole Phenyl Methanones from Substituted Anilines." Asian Journal of Organic & Medicinal Chemistry 7, no. 4 (2023): 295–98. http://dx.doi.org/10.14233/ajomc.2022.ajomc-p405.

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Triazoles, a five-membered ring structure and three nitrogen atoms, are regarded as important building blocks for the synthesis of numerous organic compounds. Triazoles and their derivatives have received considerable attention over the past decade due to their chemotherapeutic value. It’s been thought to be a functional core that exhibits most varieties of biological activity mainly antibiotics, antimicrobials and antifungals. In present work, a series of novel substituted triazole phenylmethanones were synthesized using Claisen-Schmidt condensation reaction of 1-(5-methyl-1-(substituted phen
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16

Martinez, Leandro do Nascimento, Minelly Azevedo da Silva, Aurileya de Jesus Gouveia, et al. "Microbiological and in silico evaluation of triazole and bi-triazole derivatives." Revista Eletrônica Acervo Saúde 25 (January 31, 2025): e18263. https://doi.org/10.25248/reas.e18263.2025.

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Objective: To determine the antibacterial activity of triazole and bi-triazole compounds against the pathogens Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and methicillin-resistant Staphylococcus aureus (MRSA). Methods: This targeted research was combined with in silico predictions aimed at the rational and safe screening of these compounds. For this purpose, the virtual programs Osiris, Molinspiration, and ADMETlab were used. The inhibitory potential of the compounds was evaluated by the agar dilution method and by determining the Minimum Inhibitory Concentration (
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17

Singh, Rakesh, Harpreet Kaur, and Pankaj Gupta. "1,2,3-Triazoles: Lead Molecules For Promising Drugs: A Review." Asian Journal of Chemistry 33, no. 12 (2021): 2896–918. http://dx.doi.org/10.14233/ajchem.2021.23488.

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A large number of heterocyclic compounds with five membered rings as the parent nucleus such as tetrazoles, imidazoles, triazoles, oxadiazoles, thiadiazoles, thiazoles, etc. have been studied extensively owing to their fascinating biological properties like anticancer, antifungal, antimicrobial, antitumor, anticonvulsant, antiviral, etc. 1,2,3-Triazoles are important class of five-membered biologically active heterocyclic compounds as they exhibit wide range of pharmacological activities. Triazoles are of two types viz. 1,2,3-triazole and 1,2,4-triazole. These compounds have drawn great attent
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Neelgundmath, Mahabaleshwaraiah, and Oblennavar Kotresh. "Synthesis, Evaluation and Characterization of Some 1,3,4-Triazole-2-one Derivatives as Antimicrobial Agents." E-Journal of Chemistry 9, no. 4 (2012): 2407–14. http://dx.doi.org/10.1155/2012/672125.

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A series of novel compounds like 3[(phenyl substituted)-5-methyl-1(Benzosulphonylamine)]-1,3,4-triazole-2-ones II(a-f) were synthesized by treating 4-amino-1-phenyl-3-methyl-5-oxo-1,2,4-triazoles with benzene sulphonyl chloride using pyridine as solvent. Similarly by using 4-amino-1-aryl-3-methyl-5-oxo-1,2,4-triazoles and acetic anhydride as starting material 3[(phenyl substituted)-5-methyl-1(acetylamino)]-1,3,4-triazole-2-ones III(a-f) were synthesized and also 3[(phenyl substituted)-5-methyl-1(chloroacetyl)]-1,3,4-triazole-2-ones I(a-f) were synthesized by treating 4-amino-1-aryl-3-methyl-5-
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Jansa, Petr, Petr Špaček, Ivan Votruba, et al. "Efficient one-pot synthesis of polysubstituted 6-[(1H-1,2,3-triazol-1-yl)methyl]uracils through the “click” protocol." Collection of Czechoslovak Chemical Communications 76, no. 9 (2011): 1121–31. http://dx.doi.org/10.1135/cccc2011074.

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The preparation of several triazolo acyclic nucleosides and triazolo acyclic nucleoside phosphonates is described. The synthetic methodology has been developed as an efficient one-pot Cu(I)-catalyzed azide alkyne Huisgen “click” cycloaddition. A novel Cu(I)-catalyzed decarboxylation reaction of 1-substituted 1H-1,2,3-triazole-4-carboxylic acids at room temperature was observed and used for the preparation of 1-substituted 1H-1,2,3-triazoles. As congeners of TPI (Taiho pharmaceutical inhibitor), the prepared compounds were screened as potential inhibitors of human thymidine phosphorylase, but n
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20

Shahana, Ehsan, Sarfraz Sahar, Khan Bushra, Mona Hassan Syeda, and Iqbal Munawar. "A rapid solid supported synthesis of 4-amino-5-(pyridin-4-YL)-4H-1,2,4-triazol-3-thiol and its derivatives." Chemistry International 2, no. 4 (2016): 262–66. https://doi.org/10.5281/zenodo.1471437.

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1,2,4-triazoles and its substituted derivatives were synthesized since these compounds are known for their excellent antibacterial, antifungal, anti-tubercular, antioxidant, anticancer, anti-inflammatory, analgesic, anticonvulsant and anxiolytic activities. 1,2,4-triazole and substituted derivatives of 1,2,4-triazole were synthesized using solid state microwave irradiation technique and synthesized compounds were characterized by UV-Visible, FTIR and GC-MS techniques and in future study the biological activities of synthesized compounds will be studied.
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Selezneva, Ekaterina Sergeevna, Zoya Petrovna Belousova, and Vadim Aleksandrovich Isaichkin. "The development of an adaptive response of <i>Drosophila melanogaster</i> to genotoxicity of alkyl(aryl)sulfurnyl 1,2,4-triazoles." Samara Journal of Science 11, no. 4 (2022): 121–26. http://dx.doi.org/10.55355/snv2022114118.

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The widespread use of triazoles in agriculture as retardants has led to the need to investigate the possible mutagenic effects of these compounds on natural ecosystems adjacent to agrocoenoses. Model experiments were set up to investigate the ability to induce dominant lethal mutations by synthesized triazoles: 1,2,4-triazole: (1,2,4-triazole (1,2,4-TrH), N-triazolid methanesulfonic acid (CH₃SO₂TrH), N-triazolid benzene sulfonic acid (PhSO₂1,2,4-Tr) and N-triazolid toluene sulfonic acid (4-CH₃ ArSO₂1,2,4-Tr) in Drosophila melanogaster adults. The possibility of developing an adaptive response
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22

Hricha, Joshi. "Synthetic Techniques And Pharmacological Application Of Triazole Derivatives: A Review." International Journal of Pharmaceutical Sciences 2, no. 6 (2024): 587–96. https://doi.org/10.5281/zenodo.11550285.

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There is a numerous study that have been reported as of the immense biological and pharmacological properties, there has always been an attraction from heterocyclic compound in the sector of medicinal chemistry. The triazole compounds are a key element in the area of heterocyclic chemistry and plays a role in as building blocks in both organic and medicinal chemistry. Triazole has become one of the most important heterocyclic compounds that possess characteristics of both of the natural products and medicinal compounds. Triazoles are supposed to be one of the most abundantly present compounds
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Safonov, A. A. "Synthesis, physico-chemical properties of derivatives 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-4-amine." Farmatsevtychnyi zhurnal, no. 3-4 (August 14, 2018): 50–54. http://dx.doi.org/10.32352/0367-3057.3-4.16.03.

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Recently, the search for new compounds with high biological activity, which can be the basis for potential drugs, becomes topical for world scientists. A heterocyclic compound cause particular interest in this area as highly pharmacologically active compounds. Scientists extends interest due to the low toxicity and high reactivity 1,2,4-triazole of the system. It is proved that the combination of triazole nucleus with other heterocyclic systems, especially in the fifth position, causes increased biological effect, and, sometimes, the appearance of new pharmacological activities.&#x0D; The aim
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Ohloblina, M. V. "Biological features of new 1,2,4-triazole derivatives (a literature review)." Current issues in pharmacy and medicine: science and practice 15, no. 1 (2022): 107–12. http://dx.doi.org/10.14739/2409-2932.2022.1.252305.

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Modern chemistry of 1,2,4-triazoles is in need of the search for more rational ways of synthesizing biologically active substances. To date, a number of attractive alternatives to the classical methods for the synthesis of potentially biologically active derivatives among 1,2,4-triazoles are known. The above mentioned compounds demonstrate antimicrobial, antifungal, antioxidant, anti-inflammatory, antiviral activity, etc. Based on the results of literary sources generalization, a promising direction of scientific research was chosen. The aim of this work is to determine the direction of modern
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Mohammad, Asif. "Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues." Chemistry International 1, no. 4 (2015): 174–83. https://doi.org/10.5281/zenodo.1470200.

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Various heterocyclic compounds along their derivatives were evaluated for their biological activities as antiviral, antitumor, anticonvulsant, antibacterial, antifungal, antituberculosis, analgesic, anti-inflammatory, antidiabetic, antihistamine and other biological activities. The triazole moiety seems to be very small, but in the biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. The triazole derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous
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Mohammad, Asif. "Antiviral and antiparasitic activities of various substituted triazole derivatives: A mini review." Chemistry International 1, no. 2 (2015): 71–80. https://doi.org/10.5281/zenodo.1469977.

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The presence of three nitrogen hetero-atoms in five-membered ring systems defines an interesting class of compounds, the triazole. This may be of two types, the 1,2,3-triazoles and the 1,2,4-triazoles. Out of the two triazoles, 1,2,4-triazole have drawn great attention due to its wide variety of activities, low toxicities and good pharmacokinetic and pharmacodynamic profiles. Chemistry of triazoles and their fused heterocyclic derivatives has received considerable attention owing to their effective biological activities such as anti inflammatory, analeptic, sedatives, antianxiety, antimicrobia
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Mroczyńska, Martyna, Ewelina Kurzyk, Magdalena Śliwka-Kaszyńska, Urszula Nawrot, Marta Adamik, and Anna Brillowska-Dąbrowska. "The Effect of Posaconazole, Itraconazole and Voriconazole in the Culture Medium on Aspergillus fumigatus Triazole Resistance." Microorganisms 8, no. 2 (2020): 285. http://dx.doi.org/10.3390/microorganisms8020285.

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Triazoles are the only compounds used as antibiotics in both medicine and agriculture. The presence of triazoles in the environment can contribute to the acquisition of azole resistance among isolates of Aspergillus fumigatus. The objective of this study was to investigate the effect of A. fumigatus exposure to triazoles on susceptibility to these compounds. Seventeen triazole-resistant and 21 triazole-sensitive A. fumigatus isolates were examined. The isolates were transferred 20 times on the Sabouraud medium supplemented with posaconazole, itraconazole or voriconazole, followed by five times
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Rathmann, Stephanie M., Nancy Janzen, and John F. Valliant. "Synthesis, radiolabelling, and biodistribution studies of triazole derivatives for targeting melanoma." Canadian Journal of Chemistry 94, no. 9 (2016): 773–80. http://dx.doi.org/10.1139/cjc-2016-0239.

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Molecular probes that target specific markers expressed in solid tumours are in demand for cancer imaging and radionuclide therapy applications. The synthesis, characterization, and in vivo evaluation of radioiodinated triazoles designed as probes to target melanoma are described here. Compounds were prepared using a thermal click reaction between ethynylstannane and methyl 2-azidoacetate, resulting in preferential formation of the corresponding 1,4-tin triazole. The primary amine of various targeting vectors was then coupled to the resulting tin triazole methyl ester. These precursors were la
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Cebeci, Yıldız Uygun, and Şengül Alpay Karaoğlu. "Design and microwave-assisted synthesis of a novel Mannich base and conazole derivatives and their biological assessment." Heterocyclic Communications 27, no. 1 (2021): 100–111. http://dx.doi.org/10.1515/hc-2020-0126.

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Abstract 4-Amino-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one (1) was converted to the corresponding Schiff base (2) by treatment with salicylaldehyde. 1,2,4-Triazoles were then converted to the corresponding Mannich bases containing fluroquinolone core using a one-pot three-component procedure. Moreover, the synthesis of six compounds, which can be considered as conazole analogues, was performed starting from 1,2,4-triazole-3-one compounds via three steps by either conventional or microwave-mediated conditions. All the newly synthesized compounds were screened for their antimicrobial activitie
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Jalihal, Prabhu C., Vaibhav Rajoriya, and Varsha Kashaw. "DESIGN, SYNTHESIS, AND EVALUATION OF NEW DERIVATIVE OF 1,2,4-TRIAZOLES FOR ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITY." International Journal of Current Pharmaceutical Research 10, no. 4 (2018): 29. http://dx.doi.org/10.22159/ijcpr.2018v10i4.28455.

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Objective: The object of the study is to design, synthesize and biological evaluation of isoniazid derived 1,2,4-triazoles compounds.Methods: Isoniazid based 1,2,4-triazoles derivatives have been synthesized by reaction of Isoniazid with carbon disulfide in basic medium (KOH) to form Potassium dithiocarbazinate salt and reaction with hydrazine hydrate converted into 4-amino-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol. These compounds were reacted with seven different benzaldehyde to form 4-[(substituted phenyl)-methylene]-amino-5-(pyridine-4-yl)-4H-1,2,4-triazol-3-thiol (4). The final compounds
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31

Hajri, A., D. Alimi, K. Rtibi, and H. Sebai. "Novel 6-aryl-7-alkyl/aryl-[1,2,4]triazolo[4,3-a][1,3,5]triazine-5(6H)-thiones, processes for their preparation, characterization and evaluation of their in vitro antioxidant activity." Bulletin of the Chemical Society of Ethiopia 35, no. 3 (2022): 565–72. http://dx.doi.org/10.4314/bcse.v35i3.8.

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ABSTRACT. A series of nine new 6-aryl-7-alkyl/aryl-[1,2,4]triazolo[4,3-a][1,3,5]triazine-5(6H)-thiones (2a-i) were synthesized by a reaction of N-triazol-3-yl imidates (1) with three different isothiocyanate derivatives (RNCS) in refluxing toluene. The structures of the final heterocyclic compounds were confirmed by 1H-NMR, 13C-NMR, FT-IR, elemental analysis, and mass spectral analysis. The target compounds (2a-i) were in vitro screened for their activity as antioxidants using DPPH (2,2′-diphenyl-1-picrylhydrazyl) and FRAP (ferric reducing/antioxidant power) methods. The results revealed that
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Holla, Bantwala S., Channamata S. Prasanna, Boja Poojary, Mithun Ashok, Kottapalli S. Rao, and Kanakamajalu Shridhara. "Synthesis, Characterization and Antibacterial Studies of Some 1,2,4-Triazole Derivatives Containing a 6-Chloropyridin-3-yl methyl Moiety." Zeitschrift für Naturforschung B 61, no. 3 (2006): 334–38. http://dx.doi.org/10.1515/znb-2006-0315.

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Abstract5-(6-Chloropyridin-3-yl methyl)-4-phenyl-1,2,4-triazole-3-thiol (2) and 5-substituted-4-phenyl- 1,2,4-triazole-3-thiols (3) were synthesized. Alkylation and aminomethylation reactions of these triazoles were also carried out. Some of the newly synthesized compounds were screened for their antibacterial activities.
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33

Bihdan, O. A., and V. V. Parchenko. "Synthesis and physical-chemical properties of some 5-(3-fluorophenyl)-4-methyl-1,2,4-triazole-3-thiol derivatives." Farmatsevtychnyi zhurnal, no. 2 (August 14, 2018): 38–47. http://dx.doi.org/10.32352/0367-3057.2.17.05.

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There are engaged scientists practically from all over the world to the 1,2,4-triazole system research but the greatest attention deserve the achievements of domestic scientists who managed from the very beginning to register new original medicines in Ukraine. There is no doubt that the original attempt of combining various typical fragments with the nucleus of 1,2,4-triazole is gaining popularity among researchers.&#x0D; The purpose of our work was to synthesized and investigate a row of new 5-(3-fluorophenyl)-4-methyl-1,2,4-triazole-3-thiols by a Sulfur atom, to study the physical-chemical p
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34

Choudhary, Sunil Kumar, Priya Gothwal, Nidhi Sogani, Ajay Saini, and Suman Swami. "Rational Design, Synthesis, Characterization, and Anti-bacterial activity of Urea Derivatives Bearing 1,2,4-triazoles as Molecular Hybrid Scaffolds." Oriental Journal Of Chemistry 39, no. 1 (2023): 129–35. http://dx.doi.org/10.13005/ojc/390115.

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A new set of molecular hybrids, urea derivatives carrying 1,2,4-triazole as molecular hybrid scaffolds, were developed, synthesised, characterised, and assessed for potential anti-bacterial action. Triazole scaffolds are key moieties in many pharmacological compounds, and their inclusion with urea moiety makes them more valuable for biological purposes. As a result, urea derivatives containing 1H-1,2,4-triazole and 3-(methylthio)-1H-1,2,4-triazole moieties were produced by reacting carbamates of 4-amino-1,2,4-triazoles and 3-(methylthio)-4-amino-1,2,4-triazole with amines in DMF using trimethy
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35

Loganathan, C. Geethapriya, Karthickeyan Krishnan, S. D. Vachala, Deeparani Urolagin, and J. Vijayakumar. "A Review on 1,2,3 - Triazole & Piperazine Derivatives with Various Biological Activities." Journal of Pharmaceutical Research 22, no. 3 (2023): 113–23. http://dx.doi.org/10.18579/jopcr/v22.3.23.43.

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The largest family of organic molecules in organic chemistry are heterocyclic compounds. A heterocyclic compound is created when an oxygen, nitrogen, sulphur, or atom of a similar element is included in place of a carbon atom. Heterocyclic compounds play a crucial role in daily living. It has a wide scope of uses in agrochemicals and medicinal chemistry. One of a pair of chemical compounds known as triazoles and Piperazine, with the molecular formula C2H3N3 and C5H5N. A fundamental aromatic heterocyclic scaffold is 1,2,3-triazole and piperazine. Because of its structural characteristics, these
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Lelyukh, Maryan, Arkady Savchenko, Myroslava Kalytovska, et al. "Pharmacological profile of condensed heterocyclic compounds based on functionally substituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles: A review." Current Chemistry Letters 14, no. 3 (2025): 567–78. https://doi.org/10.5267/j.ccl.2025.3.001.

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Triazolo[3,4-b][1,3,4]thiadiazole molecules are found to be important tools in modern bioorganic and medicinal chemistry. This condensed system successfully combines two pharmacologically significant five-membered heterocycles – 1,2,4-triazole and 1,3,4-thiadiazole, which causes much more interest in the enhanced activity profile of its analogs than their parent separate constituents. It’s considered that the triazoles fused to thiadiazoles exhibit various therapeutically important properties, probably due to the existence of N-C-S fragments in their structures. In this review, we presented th
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Pandey, Vinod Kumar, Zehra Tusi, Sumerah Tusi, and Madhawanand Joshi. "Synthesis and Biological Evaluation of Some Novel 5-[(3-Aralkyl Amido/Imidoalkyl) Phenyl]-1,2,4-Triazolo[3,4-b]-1,3,4-Thiadiazines as Antiviral Agents." ISRN Organic Chemistry 2012 (September 11, 2012): 1–7. http://dx.doi.org/10.5402/2012/760517.

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A series of novel 4-amino-5-mercapto-3-[(3-aralkyl amido/imidoalkyl) phenyl]-1,2,4-triazoles (5a-d) were obtained by treating m-(aralkyl amido/imidoalkyl) benzoic acid hydrazides (3a-d) with carbon disulphide in alcoholic KOH and hydrazine hydrate, respectively. These triazole derivatives were employed in the synthesis of 5-[(3′-aralkyl amido/imidoalkyl) phenyl]-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines (6a-d). The newly synthesized compounds were evaluated for their antiviral activity against two animal viruses, namely, Japanese encephalitis virus (JEV) strain P20778 and herpes simplex virus-1
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Fedotov, S. O., and A. S. Hotsulia. "Synthesis and properties of 3-(ethylthio)-9-methyl-6-(alkylthio)pyrazolo[1,5-d][1,2,4]triazolo[3,4-f][1,2,4]triazines." Current issues in pharmacy and medicine: science and practice 15, no. 3 (2022): 227–34. http://dx.doi.org/10.14739/2409-2932.2022.3.263994.

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The combination of pyrazole and 1,2,4-triazole fragments in one structure makes it possible to achieve some success in creating potential biologically active compounds. Various factors contribute to this process. Among them, we can note the significant possibilities of chemical transformation involving these cycles, the simplicity, and reliability of methods, the creation of molecules with a certain level of bioavailability and the ability to influence a number of biochemical processes. Taking into account the presented facts, the creation of new compounds in a number of pyrazolo-triazole cond
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39

Karpun, E. O., and V. V. Parchenko. "Synthesis, physicochemical properties and antigypoxic activity of some S-derivatives of 4-alkyl-5-(((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol." Farmatsevtychnyi zhurnal, no. 6 (December 9, 2020): 56–64. http://dx.doi.org/10.32352/0367-3057.6.20.06.

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Hypoxia is a discrepancy between the required energy of the cell in the mitochondrial oxidative phosphorylation system. The immediate cause of the deficiency is a decrease in the oxygen concentration in the mitochondria. Today there is a huge demand for the development of new anti-hypoxic drugs. t is known that 1,2,4-triazole compounds can have antimicrobial, anti-inflammatory, anti-hypoxic effects. Modification of the 1,2,4-triazole nucleus is a productive way to create original active molecules with a non-planar structure, for their binding to bio-target substrates. Derivatives of bis-1,2,4-
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Kishor, Raval* Kaushik Patel Shivani Patel Ronak Patel Snehal Patel. "A Review On 1,2,4-Triazoles." Journal of Pharma Research 1, no. 1 (2012): 1–4. https://doi.org/10.5281/zenodo.1098645.

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<strong><em>ABSTRACT</em></strong> <em>Triazole is a five membered heterocyclic system consisting of two carbon atoms and three nitrogen atoms shows wide range of biological activities. Triazoles can be synthesized using Einhorn-Brunner reaction or the Pellizzari reaction from acyl hydrazides and various different method. Triazole derivatives are showing very promising and excellent therapeutic effectiveness. The major activities exhibited by these derivatives include insecticial, antifungal, antiviral, antibacterial, sedative,hypnotic, anticonvulsant and anti-inflammatory action. In recent ye
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41

Caiana, Rodrigo Ribeiro Alves, Cosme Silva Santos, Ronaldo Nascimento de Oliveira, and Juliano Carlo Rufino Freitas. "Scientific and Technological Prospecting of 1H-1,2,3-Triazoles." Current Organic Chemistry 26, no. 3 (2022): 275–86. http://dx.doi.org/10.2174/1385272826666220126153429.

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Abstract: The use of 1H-1,2,3-triazoles has become an important scaffold for applications in different technological sectors. Therefore, we sought to carry out technological monitoring to understand the international scenario involving 1H-1,2,3-triazoles from the patents filed, in addition to evaluating the relationship between the growth in the number of patents and the improvement of strategies for obtaining these compounds via a metal-catalyzed azide-alkyne cycloaddition reaction. Technological monitoring was performed with the support of the PatentInspiration ® platform, using the keywords
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42

Dovbnya, Dmytro V., Andrii G. Kaplaushenko, and Alla S. Korzhova. "Synthesis and alkylation of 5-aryl-1,2-dihydro-3H-1,2,4-triazole-3-thiones." Journal of Organic and Pharmaceutical Chemistry 19, no. 2(74) (2021): 53–59. http://dx.doi.org/10.24959/ophcj.21.188135.

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5-R-1,2,4-triazole-3-thiones and their derivatives are easy to obtain; they have low toxicity and a broad spectrum of the biological activity. It makes this class of heterocyclic compounds promising for creating potential drugs. Aim. To develop the preparative methods for the synthesis of 5-aryl-1,2-dihydro-3H-1,2,4-triazole-3-thiones and study their reactivity in the alkylation reaction. Results and discussion. New 5-aryl-1,2-dihydro-3H-1,2,4-triazole-3-thiones were synthesized. The latter were used for the synthesis of 3-aryl-5-(alkylthio)-4H-1,2,4-triazoles. Experimental part. Using a serie
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43

Safonov, A. A., and O. I. Panasenko. "Synthesis, antimicrobial and antifungal activity of 3-(2-bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles." Current issues in pharmacy and medicine: science and practice 15, no. 3 (2022): 235–40. http://dx.doi.org/10.14739/2409-2932.2022.3.264691.

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To select a molecule that could become a promising pharmacological agent, chemists use already-known heterocyclic bases by adding pharmacologically active groups. One such heterocyclic system is 1,2,4-triazole base, on the basis of which a huge number of biologically active compounds have already been found. It is known that 1,2,4-triazole derivatives show a fairly high antimicrobial and antifungal effect while remaining low-toxic compounds and 5-alkylthio-1,2,4-triazoles exhibit antimicrobial and antifungal activity. Based on the literature search, it can be concluded that 3-(2-bromophenyl)-5
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44

Rawat, Rhambus, Prem Shankar Deo, and Bhushan Shakya. "Synthesis, Characterization and Study of Antimicrobial Activities of Mannich Bases Incorporating 1,2,4-Triazole Nucleus." Amrit Research Journal 2, no. 01 (2021): 19–27. http://dx.doi.org/10.3126/arj.v2i01.39894.

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Heterocyclic compounds containing triazole moiety have great importance in the field of medicine, pharmaceuticals, biochemistry, biology, therapeutics, environmental science, and industry. Triazoles and their derivatives have been extensively used in the development of new drugs. Biological activities of Schiff bases are highly investigated, but Mannich bases are on the verge of their development, and they are being synthesized in large number nowadays. In this work, Mannich bases are synthesized by incorporation 1,2,4-triazole moiety through Schiff base using different amines. Mannich bases a
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Оглобліна, М. В., І. В. Бушуєва, and В. В. Парченко. "Review of the research on the influence of different functional substituents of new 1,2,4-triazole derivatives on the compounds biological properties." Farmatsevtychnyi zhurnal, no. 5 (October 29, 2022): 74–80. http://dx.doi.org/10.32352/0367-3057.5.22.08.

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Today, 1,2,4-triazole derivatives are a promising class of organic compounds. This is caused, first of all, by the possibility of various chemical modifications of the 1,2,4-triazole fragment due to the addition of typical pharmacophores, which contributes to the expansion of the new molecules’ arsenal. A significant number of the 1,2,4-triazole derivatives show biological properties, that postively affects the further process of the most promising substances’ introduction.&#x0D; The aim of the work was to analyze the influence of various functional substituents of the new 1,2,4-triazole deriv
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46

Khan, Ayad Kareem. "Facile Synthesis, Characterization of New Quinazolinones with Different Azo Compounds, 1,2,3-Triazole Moieties and Evaluation Their Anti-bacterial Activity." Al-Mustansiriyah Journal of Science 28, no. 3 (2018): 122. http://dx.doi.org/10.23851/mjs.v28i3.180.

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In the present research, a series of some azo compounds (5-9) and 1,2,3-triazoles derived from 2-methyl quinazolin-4(3H)-one were synthesized successfully by stepwise routes includes the following: 3-amino-2-methylquinazolin-4(3H)-one (3) prepared firstly by conversion of 2-aminobenzoic acid into methyl 2-aminobenzoate (1) followed by reaction with acetic anhydride to form methyl -2-acetamidobenzoate (2). The amide then allowed reacting with hydrazine hydrate to give compound (3). Diazotization reaction with sodium nitrite in the presence of hydrochloric acid yield the 3-(chlorodiazenyl)-2-met
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47

Nakahata, Masaki, and Akihito Hashidzume. "Density Function Theory Study on the Energy and Circular Dichroism Spectrum for Methylene-Linked Triazole Diads Depending on the Substitution Position and Conformation." Molecules 29, no. 12 (2024): 2931. http://dx.doi.org/10.3390/molecules29122931.

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Since the discovery of metal-catalyzed azide–alkyne cycloadditions, 1,2,3-triazoles have been widely used as linkers for various residues. 1,2,3-Triazole is an aromatic five-membered cyclic compound consisting of three nitrogen and two carbon atoms with large dipoles that absorb UV light. In the past decade, we have been working on the synthesis of dense triazole polymers possessing many 1,2,3-triazole residues linked through a carbon atom in their backbone as a new type of functional polymer. Recently, we reported that stereoregular dense triazole uniform oligomers exhibit a circular dichrois
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48

Wang, Huanhong, Xiaofei Yi, Yanli Cui, and Wanzhi Chen. "Rhodium-catalyzed triazole-directed C–H bond functionalization of arenes with diazo compounds." Organic & Biomolecular Chemistry 16, no. 43 (2018): 8191–95. http://dx.doi.org/10.1039/c8ob01673a.

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Shafique, Kainat, Aftab Farrukh, Tariq Mahmood Ali, et al. "Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives." Molecules 28, no. 7 (2023): 3104. http://dx.doi.org/10.3390/molecules28073104.

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In the present study, a new series of 1,2,3-triazole derivatives was synthesized via a click one-pot reaction. The synthesized compounds were found to be active during molecular docking studies against targeted protein 1T69 by using the Molecular Operating Environment (MOE) software. The designed and synthesized compounds were characterized by using FT-IR, 1H-NMR and LC-MS spectra. The synthesized triazole moieties were further screened for their α-amylase and α-glucosidase inhibitory activities. The preliminary activity analysis revealed that all the compounds showed good inhibition activity,
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50

Singh, Ram Janam, and Dharmendra Kumar Singh. "Novel Syntheses of Some 1, 2, 4-Triazoles as Potent Bacteriocidal Agents." E-Journal of Chemistry 7, no. 1 (2010): 37–40. http://dx.doi.org/10.1155/2010/168651.

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A facile syntheses of 4-aryl-5-(isomeric pyridoyl)-3H-1, 2, 4-triazoles as potent bacteriocidal agents are described. The newly synthesized compounds were characterized by spectral and elemental analyses. Some compounds were screened for their antibacterial activity againstS. aureus, E. coli, B. subtilisandP.aeruginosa.All compounds carrying 1, 2, 4- triazole moiety showed significant biological activity
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