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Journal articles on the topic '1;2;4-triazole derivatives'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

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> 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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2

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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3

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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4

Murthy Appala, Venkata Ramana, Kanaka Durga Bhavani Anagani, and Aparna Pasula. "Synthesis of New Piperidine based N(2)-Alkylated 1,2,3-Triazole Hybrids in Basic Medium." Asian Journal of Chemistry 35, no. 1 (2022): 212–16. http://dx.doi.org/10.14233/ajchem.2023.26906.

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The nucleophilic reaction of 1H-triazole derivatives with piperidines under basic conditions is the essential step in the synthesis of a new series of dibenzyl N(2)-C-linked triazolyl piperidines. The triazole derivative was synthesized via the CuAAc reaction of 1-phenylprop-2-yn-1-ol (1a-b) with azidomethyl pivalate. Compound 3a-b underwent dehydroxylation and deprotection reactions using TFA, triethyl silane and 1 M NaOH respectively, yielding monobenzyl 1H-1,2,3-triazole (4a-b). The N(2)-piperidinyltriazoles (6a-j) were synthesized in significant amounts by nucleophilically reacting 1H-tria

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5

*Prytula, R. L., V. V. Parchenko, I. V. Bushuyeva, O. K. Yerenko, and T. V. Khortetska. "DESIGN, SYNTHESIS, AND BIOLOGICAL PROPERTIES OF NEW 1,2,4-TRIAZOLE DERIVATIVES." World Journal of Pharmaceutical Science and Research 3, no. 5 (2024): 220–28. https://doi.org/10.5281/zenodo.13903664.

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For a long time, derivatives of 1,2,4-triazole have attracted the attention of scientists worldwide. Their unique and valuable properties provide researchers with information on the practically limitless possibilities for discovering new promising molecules. The biological potential of 1,2,4-triazole derivatives is also well-known and is not limited to antifungal and antimicrobial properties. Many new types of pharmacological activity of substituted 1,2,4-triazoles have been discovered and studied by scientists over the past ten years. Regarding the general methods of synthesizing 1,2,4-triazo

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6

Shakeel Ahmed, Shiza Murad, Iqra Munir, et al. "Spectroscopic Investigation and Synthesis of N-Ethyl-5-Tolyloxymethyl Triazole Derivatives." Indus Journal of Bioscience Research 3, no. 5 (2025): 288–96. https://doi.org/10.70749/ijbr.v3i5.1234.

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High-nitrogen heterocycles' synthesis has attracted much interest because of their wide applicability in many different sectors. As a significant class of organic compounds, triazoles and their fused derivatives have emerged among these. A new triazole derivative, 4-ethyl-3-ethylthio-5-(p-tolyloxymethyl)-4H-1, 2, 4-triazole, is the subject of this work on synthesis and spectrum characterization. Ethyl 2-p-tolyloxy acetate is synthesized by reacting 3, 4-dimethoxyphenylacetic acid with ethanol under concentrated H2SO4, starting the process. The ester product is subsequently transformed into 2-p

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7

Sabzi, Noor Ali Hussein, and May Mohammed Jawad Al-Mudhafar. "Synthesis, characterization, and antimicrobial evaluation of new Schiff bases derived from vanillic acid conjugated to heterocyclic 4H-1,2,4-triazole-3-thiol." Pharmacia 70, no. (3) (2023): 657–63. https://doi.org/10.3897/pharmacia.70.e104579.

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A multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (4). Finally, several aromatized aldehydes reacted with compound (4) to produce Schiff bases derivatives (5–11). The purpose of this research is to prepare new vanillic acid derivatives with 1, 2, 4-triazole-3-thiol heterocyclic ring structures and to evaluate their antimicrobial activity in a preliminary assessment. Fourier-transform infrared (FT-IR) and proton nuclear magnetic resonance spectroscopy (<sup>1</sup>H-NMR) were used to verify the structures of the newly synthesize

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8

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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9

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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10

Ihnatova, Tetiana, Andriy Kaplaushenko, Yuliia Frolova, and Evheniy Pryhlo. "Synthesis and antioxidant properties of some new 5-phenethyl-3-thio-1,2,4-triazoles." Pharmacia 68, no. (1) (2021): 129–33. https://doi.org/10.3897/pharmacia.68.e53320.

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Novel derivatives of 4-R-5-phenethyl-4H-1,2,4-triazole-3-thiols were synthesized. The proposed approaches and developed synthetic protocols provided the possibility to design 4-R-5-phenethyl-4H-1,2,4-triazole-3-thiols and their derivatives have been shown. The antioxidant activity of the synthesized compounds was evaluated in vitro by the method of the non-enzymatic initiation of BOD with salts of iron (II). When compared with existing antioxidants, some of our compounds were found to be more potent.

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11

Nurmaganbetov, Zhangeldy S., Oralgazy A. Nurkenov, Andrei I. Khlebnikov, et al. "Antiviral Activity of (1S,9aR)-1-[(1,2,3-Triazol-1-yl)methyl]octahydro-1H-quinolizines from the Alkaloid Lupinine." Molecules 29, no. 23 (2024): 5742. https://doi.org/10.3390/molecules29235742.

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Influenza is a disease of significant morbidity and mortality. The number of anti-influenza drugs is small; many of them stimulate the appearance of resistant strains. This article presents the results of assessing the antiviral activity of 1,2,3-triazole-containing derivatives of alkaloid lupinine for their ability to suppress the reproduction of orthomyxoviruses (influenza viruses: A/Vladivostok/2/09 (H1N1) and A/Almaty/8/98 (H3N2)). The ability of (1S,9aR)-1-[(1,2,3-triazol-1-yl)-methyl]octahydro-1H-quinolizines with aryl-, 4-((4-formylphenoxy)methyl)- or 4-((3-tert-butyl-5-ethyl-2-hydroxy-

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12

Janam Singh, Ram, and Dharmendra Kumar Singh. "Syntheses of Some 3,5-Diaryl-4H-1,2,4-triazole Derivatives and their Antifungal Activity." E-Journal of Chemistry 6, s1 (2009): S219—S224. http://dx.doi.org/10.1155/2009/925964.

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Syntheses of a series of 3, 5-diaryl-4H-1, 2, 4-triazole derivatives are described. In this present work, 4-amino-3-phenyl-5-p-tolyl-4H-1,2,4-triazole(1) was converted toN,N’-bis[3-phenyl-5-p-tolyl-4H-1,2,4-triazolyl]-1,4-xylenediimine(2) and 3-Phenyl-5-p-tolyl-4-[4-methyl benzylidenamino]-4H-1,2,4-triazole (3) in good yields by treatment with aldehydes OHC-C6H4-CHO and Ar-CHO respectively. The compoundsN,N’-bis[3-phenyl-5-p-tolyl-4H-1,2,4-triazolyl]-1,4-xylenediimine (2) and 3-phenyl-5-p-tolyl-4-[4-methyl benzylidenamino]-4H-1,2,4-triazole (3) were reduced with NaBH4to afford the correspondin

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13

Dobosz, Maria, Monika Pitucha, Izabela Dybala, and Anna E. Kozioł. "Cyclization of Semicarbazide Derivatives of 3-Methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-4-acetic Acid." Collection of Czechoslovak Chemical Communications 68, no. 4 (2003): 792–800. http://dx.doi.org/10.1135/cccc20030792.

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By the reaction of hydrazide of 3-methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-4-acetic acid (1) with isocyanates, 3-methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-4-acetosemicarbazide derivatives 2 were obtained. Cyclization of these compounds in the presence of 2% NaOH led to the formation of 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives 3, which was confirmed by X-ray analysis of 3b.

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14

Kazeminejad, Zahra, Mahrokh Marzi, Abolfazl Shiroudi, Seyed Amin Kouhpayeh, Mojtaba Farjam, and Elham Zarenezhad. "Novel 1, 2, 4-Triazoles as Antifungal Agents." BioMed Research International 2022 (March 22, 2022): 1–39. http://dx.doi.org/10.1155/2022/4584846.

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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 mos

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15

Xiao, Pan-Lei, Xiu-Ying Song, Xin-Ting Xiong, Da-Yong Peng, and Xu-Liang Nie. "Synthesis, Crystal Structure, Spectral Characterization and Antifungal Activity of Novel Phenolic Acid Triazole Derivatives." Molecules 28, no. 19 (2023): 6970. http://dx.doi.org/10.3390/molecules28196970.

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At present, phenolic acid derivatives and triazole derivatives have a good antifungal effect, which has attracted widespread attention. A series of novel phenolic acid triazole derivatives were synthesized, and their structures were characterized by IR, MS, NMR, and X-ray crystal diffraction. Compound methyl 4-(2-bromoethoxy)benzoate, methyl 4-(2-(1H-1,2,4-triazol-1-yl) ethoxy)benzoate, 4-(2-(1H-1,2,4-triazol-1-yl)ethoxy)benzoic acid and 4-(2-(1H-1,2,4-triazol-1-yl) ethoxy)-3-methoxybenzoic acid crystallize in the monoclinic system with space group P21/n, the monoclinic system with space group

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16

Singh, R. J., and D. K. Singh. "Syntheses, Characterization and Biological Activity of Some 1, 2, 4-Triazole Derivatives." E-Journal of Chemistry 6, no. 3 (2009): 796–800. http://dx.doi.org/10.1155/2009/419214.

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Syntheses of a series of 3-alkyl-4- amino-5- cyanomethyl-4H-1, 2, 4-triazoles with active methylene groups 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. subtilis and P. aeruginosa. All the compounds carrying 1, 2, 4- triazole moiety showed significant biological activity.

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17

Maliszewska-Guz, Alicja, Monika Wujec, Monika Pitucha, et al. "Cyclization of 1-{[(4-Methyl-4H-1,2,4-triazol-3-yl)sulfanyl]acetyl}thiosemicarbazides to 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives and Their Pharmacological Properties." Collection of Czechoslovak Chemical Communications 70, no. 1 (2005): 51–62. http://dx.doi.org/10.1135/cccc20050051.

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By the reaction of 4-methyl-4H-1,2,4-triazole-3-thiol with ethyl bromoacetate, ethyl [(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]acetate (1) was obtained. This compound was converted to [(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]acetohydrazide (2). In the reaction of 2 with isothiocyanates, new thiosemicarbazides 3a-3g were obtained. The cyclization of 3a-3g in 2% aqueous solution of sodium hydroxide led to the formation of 4H-1,2,4-triazole-3(2H)-thione derivatives 4a-4g, whereas the cyclization in acid media led to the formation of 2-amino-1,3,4-thiadiazole derivatives 5a-5g. Molecular structur

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18

Nahlé, A., R. Salim, F. El Hajjaji, et al. "Novel triazole derivatives as ecological corrosion inhibitors for mild steel in 1.0 M HCl: experimental & theoretical approach." RSC Advances 11, no. 7 (2021): 4147–62. http://dx.doi.org/10.1039/d0ra09679b.

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The present paper illustrates the investigation of two novel ecological triazole derivative corrosion inhibitors, namely ethyl 2-(4-phenyl-1H-1,2,3-triazol-1-yl) acetate [Tria-CO<sub>2</sub>Et], and 2-(4-phenyl-1H-1,2,3-triazol-1-yl) acetohydrazide [Tria-CONHNH<sub>2</sub>].

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19

Reeta, Tripathi, Mishra Diwa, and Singh Arun. "Preparation and Antimicrobial Studies of Oxadiazine Containing Heterocyclic Compounds." International Journal of Trend in Scientific Research and Development 3, no. 5 (2019): 412–14. https://doi.org/10.5281/zenodo.3589858.

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The triazole derivative say 2 3 methylthio 5 phenyl 4H 1,2,4 triazol 4 yl acetohydrazide 1 was prepared. Various Schiff bases 3a e of 1 were prepared by reacting with various benzaldehyde derivatives 2a e . All the 3a e compounds condensed with benzoyl isothiocyanate 4 to afford N 2 aryl 6 phenyl 4 thioxo 2H 1,3,5 oxadiazin 3 4H yl 2 3 methylthio 5 phenyl 4H 1,2,4 triazol 4 yl acetamide derivatives 5a e . All the synthesized compounds characterized spectroscopically and tested for antimicrobial activity. Reeta Tripathi | Diwa Mishra | Arun Singh "Preparation and Antimicrobial Studies of O

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20

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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21

Sabzi, Noor Ali Hussein, and May Mohammed Jawad Al-Mudhafar. "Synthesis, characterization, and antimicrobial evaluation of new Schiff bases derived from vanillic acid conjugated to heterocyclic 4H-1,2,4-triazole-3-thiol." Pharmacia 70, no. 3 (2023): 657–63. http://dx.doi.org/10.3897/pharmacia.70.e104579.

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A multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (4). Finally, several aromatized aldehydes reacted with compound (4) to produce Schiff bases derivatives (5–11). The purpose of this research is to prepare new vanillic acid derivatives with 1, 2, 4-triazole-3-thiol heterocyclic ring structures and to evaluate their antimicrobial activity in a preliminary assessment. Fourier-transform infrared (FT-IR) and proton nuclear magnetic resonance spectroscopy (1H-NMR) were used to verify the structures of the newly synthesized compounds

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22

Journal, Baghdad Science. "Synthesis of Some Heterocyclic Compounds Derived from 2-Mercapto Benzoxazole." Baghdad Science Journal 10, no. 3 (2013): 766–78. http://dx.doi.org/10.21123/bsj.10.3.766-778.

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New series of 2-mecapto benzoxazole derivatives (1-20) incorporated into fused to different nitrogen and suphur containing heterocyclic were prepared from 2-meracpto benzoxazole, when treated with hydrazine hydrate to afford 2-hydrazino benzoxazol (1). Compound (1) converted to a variety of pyridazinone andphthalazinone derivatives (2-4) by reaction with different carboxylic anhydride. Also, reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-phenyl-1,3-thiazolidin-2,4-dione-2-(benzoxazole-2-yl-hydrazone) (6). Azomethines (7-10) were prepared through reaction of (1)

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23

Askar, Firyal W., Huda A. Hassan, and Nahida A. Jinzeel. "Synthesis of Some Heterocyclic Compounds Derived from 2-Mercapto Benzoxazole." Baghdad Science Journal 10, no. 3 (2013): 766–78. http://dx.doi.org/10.21123/bsj.2013.10.3.766-778.

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New series of 2-mecapto benzoxazole derivatives (1-20) incorporated into fused to different nitrogen and suphur containing heterocyclic were prepared from 2-meracpto benzoxazole, when treated with hydrazine hydrate to afford 2-hydrazino benzoxazol (1). Compound (1) converted to a variety of pyridazinone andphthalazinone derivatives (2-4) by reaction with different carboxylic anhydride. Also, reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-phenyl-1,3-thiazolidin-2,4-dione-2-(benzoxazole-2-yl-hydrazone) (6). Azomethines (7-10) were prepared through reaction of (1)

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24

Gribanov, Pavel S., Anna N. Philippova, Alexander F. Smol’yakov, et al. "Synthesis of Functionalized 1H-Imidazoles via Denitrogenative Transformation of 5-Amino-1,2,3-Triazoles." Molecules 30, no. 7 (2025): 1401. https://doi.org/10.3390/molecules30071401.

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An efficient access to novel 2-substituted 1H-imidazole derivatives was developed based on acid-mediated denitrogenative transformation of 5-amino-1,2,3-triazole derivatives available through dipolar azide−nitrile cycloaddition (DCR). The proposed approach includes intramolecular cyclization of 5-amino-4-aryl-1-(2,2-diethoxyethyl) 1,2,3-triazoles followed by triazole ring opening and insertion of in situ formed carbene intermediate into the O-H bond of different alcohols under acidic conditions.

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25

Makhova, N. N., I. V. Ovchinnikov, A. S. Kulikov, S. I. Molotov, and E. L. Baryshnikova. "Monocyclic and cascade rearrangements of furoxans." Pure and Applied Chemistry 76, no. 9 (2004): 1691–703. http://dx.doi.org/10.1351/pac200476091691.

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Monocyclic rearrangements of azoles are extensively studied as alternative methods for the preparation of new heterocyclic systems. The present work is devoted to investigation of monocyclic and cascade rearrangements of 1,2,5-oxadiazole 2-oxide (furoxan) derivatives. It was found during investigations that rearrangements of furoxan ring had some peculiarities in comparison with analogous rearrangements of other azoles. Therefore, three different kinds of rearrangements were found. The first of them occurred through a dinitroso-ethylene intermediate and resulted in the synthesis of 1,2,3-triaz

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26

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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27

Tashrifi, Zahra, Maryam Mohammadi-khanaposhtani, Mehdi Shafiee Ardestani, et al. "Design, Synthesis and In vitro Cytotoxicity of New 1,2,3-triazol- and Nitrostyrene Hybrids as Potent Anticancer Agents." Letters in Drug Design & Discovery 16, no. 2 (2018): 213–19. http://dx.doi.org/10.2174/1570180815666180427151830.

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Background: A new series of 1,2,3-triazol-nitrostyrene derivatives was designed, synthesized, and evaluated for cytotoxic activity against Hep-2 and L929 cell lines. </P><P> Methods: The synthetic procedure started from the functionalization of 4-hydroxybenzaldehyde with propargyl bromide and a subsequent click reaction to give 1,2,3-triazole derivatives. Then, the reaction of the mentioned derivatives with nitromethane led to the formation of the title compounds in excellent yields. Results: Most of the compounds exhibited better cytotoxic activity with respect to the standard dru

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28

D., R. Godhani, M. Sanghani A., B. Sanja D., and B. Dobariya P. "Synthesis and antimicrobial elucidation of [1,2,4]-triazole-3-thione derivatives." Journal of Indian Chemical Society Vol. 89, Jul 2012 (2012): 971–74. https://doi.org/10.5281/zenodo.5767111.

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Department of Chemistry, Mahatma Gandhi Campus, Bhavnagar University, Bhavnagar-364 022, Gujarat, India <em>E-mail </em>: drgodhani@yahoo.com <em>Manuscript received 02 November 2()10, revised 14 September 2011, accepted 08 November 2011</em> 4-Nitro benzoyl isothiocyanate (1) is prepared by a reaction of 4-nitro benzoyl chloride and ammonium isothiocyanate. Compound 1 reacts with phenyl hydrazine in the presence of acetone to form 5-(4-nitrophenyl)-l-phenyi-1<em>H</em>-1,2,4-triazole-3(2<em>H</em>)-thione (2). Compounds 2 on reaction with formaldehyde and different aromatic amines in 1,4- dio

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29

Alkhaldi, Abdulsalam A. M., Mohamed A. Abdelgawad, Bahaa G. M. Youssif, Ahmed O. El-Gendy, and Harry P. De Koning. "Synthesis, antimicrobial activities and GAPDH docking of novel 1, 2, 3-triazole derivatives." Tropical Journal of Pharmaceutical Research 18, no. 5 (2021): 1101–8. http://dx.doi.org/10.4314/tjpr.v18i5.27.

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Purpose: To synthesize new triazole derivatives in order to overcome the problem of side effects of antimicrobial agents and microbial resistance, while broadening the spectrum of antimicrobial activity. Methods: The starting triazole, compound 1, was prepared through click chemistry and reacted with chloroacetyl chloride to yield compound II. Triazole 1 was reacted with acids and aldehydes to produce oxadiazole (III) and azomethine (IV) which cyclized in acetic anhydride to give a new acetylated oxadiazole (V). Minimum inhibitory concentration (MIC) and resorufin assays were used for an

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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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Safonov, A. A., and I. S. Nosulenko. "Antiradical activity of novel 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol derivatives." Current issues in pharmacy and medicine: science and practice 14, no. 2 (2021): 162–66. http://dx.doi.org/10.14739/2409-2932.2021.2.230129.

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The process of studying free radicals began in the middle of the last century (the free radical theory of aging in 1956). Multiple studies have revealed the effect of free radicals on the cells of the body and the development of various diseases, such as diabetes, autoimmune diseases, diseases of the nervous system, and others. As a result, the term antioxidant has emerged, compounds that reduce and prevent the effects of free radicals. Most of the newly synthesized substances are studied for their antiradical properties. 1,2,4-Triazole derivatives are no exception, which has already proven th

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Artime, Mirian, Alfonso Castiñeiras, Isabel García-Santos, and Manuel Saa. "Structural Study of Three 1,2,4-triazole Derivatives Prepared by Oxidative Cyclization of Thiosemicarbazides." Proceedings 9, no. 1 (2018): 20. http://dx.doi.org/10.3390/ecsoc-22-05852.

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In the present research, 5,5-dimethyl-4-phenyl-4,5-dihydro-3H-1,2,4-triazole-3-thione (1) was prepared by condensation from N-phenylhydrazinecarbothioamide, while 4-phenyl-5-(pyrazin-2-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione (2) and 2-((5-(pyridin-2-yl) -4H-1,2,4-triazol-3-yl)thio)acetic acid (3) was prepared by oxidative cyclization from 2-(amino(pyrazin-2-yl)methylene)-N-phenylhydrazine-1-carbothioamide and 2-(amino(pyridine-2-yl)methylene)hydrazine-1-carbothioamide, respectively. The three compounds have been well characterized and their molecular structures studied by single-crystal X-r

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Afrough, T., M. Bakavoli, and H. Eshghi. "Synthesis and characterisation of new 3-methyl-6-[1-(pyrimidin-4-yl)ethyl]-5H-pyrimido[5,4-e][1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives." Journal of Chemical Research 41, no. 7 (2017): 376–79. http://dx.doi.org/10.3184/174751917x14967701766978.

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A new series of 3-methyl-6-[1-(pyrimidin-4-yl)ethyl]-5 H-pyrimido[5,4- e][1,2,4]triazolo[3,4- b][1,3,4]thiadiazine derivatives was synthesised through the condensation reaction of 5-bromo-4-[1-(5-bromo-2,6-dichloropyrimidin-4-yl)ethyl]-2-chloro-6-methylpyrimidine and 4-amino-5-methyl-4 H-1,2,4-triazole-3-thiol.

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Chakraborty, Anup K., Namrata Patel, Sarita Karole, and Kavita R. Loksh. "Design, synthesis and anticancer activity studies of some novel 1,2,4 triazole pyridine derivatives." International Journal of Pharmaceutical Chemistry and Analysis 9, no. 1 (2022): 56–61. http://dx.doi.org/10.18231/j.ijpca.2022.009.

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The development of new anticancer agents is one of the most pressing research areas in medicinal chemistry and medicine. The importance of triazole and pyridine rings as scaffolds present in a wide range of therapeutic agents has been well reported and has driven the synthesis of a large number of novel anticancer agents. The presence of these heterocyclic furnishes extensive synthetic possibilities due to the presence of several reaction sites. Prompted by these data we designed, synthesized and evaluated a series of novel 1, 2, 4-triazole-pyridine hybrid derivatives as potential anticancer a

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Danilkina, Natalia A., Nina S. Bukhtiiarova, Anastasia I. Govdi, et al. "Synthesis and Properties of 6-Aryl-4-azidocinnolines and 6-Aryl-4-(1,2,3-1H-triazol-1-yl)cinnolines." Molecules 24, no. 13 (2019): 2386. http://dx.doi.org/10.3390/molecules24132386.

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An efficient approach towards the synthesis of 6-aryl-4-azidocinnolines was developed with the aim of exploring the photophysical properties of 6-aryl-4-azidocinnolines and their click reaction products with alkynes, 6-aryl-4-(1,2,3-1H-triazol-1-yl)cinnolines. The synthetic route is based on the Richter-type cyclization of 2-ethynyl-4-aryltriazenes with the formation of 4-bromo-6-arylcinnolines and nucleophilic substitution of a bromine atom with an azide functional group. The developed synthetic approach is tolerant to variations of functional groups on the aryl moiety. The resulting azidocin

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Journal, Baghdad Science. "Synthesis and Characterization of Some New Morpholine Derivatives." Baghdad Science Journal 13, no. 2 (2016): 253–65. http://dx.doi.org/10.21123/bsj.13.2.253-265.

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In this paper a new series of morpholine derivatives was prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as a catalyst in benzene gave morpholin-N-ethyl acetate(1) which reacted with hydrazine hydrate in ethanol, and gave morpholin-N-ethyl acetohydrazide (2) . Morpholin-N-aceto semithiocarbazide (3) were prepared by reacting compound(2) with ammonium thiocyanate , concentrated hydrochloric acid and ethanol as a solvent .Compound (3) reacted with sodium hydroxide and hydrochloric acid to give 5-(morpholin-N-methylene)-1H-1,2,4-triazole-3-thiol (4) .Th

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Darehkordi, Ali, and Somayeh Ghazi. "Synthesis of a New Class of Tris- and Bis(1,3,4-thiadiazol-2-amine) Methyl and Ethyl Tris- and Bis-2-(2-(2-benzoyl hydrazinyl)-4-oxothiazolidine) Acetate Derivatives." Journal of Chemistry 2013 (2013): 1–8. http://dx.doi.org/10.1155/2013/857956.

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Hydrazine, carbothioamide derivatives2,3, and4were synthesized by the condensation of 1, 3, 5-tri carbonyl tri chloride, Terephthaloyl dichloride, and 1, 4-dicarbonyl chloride with thiosemicarbazide in presence of pyridine as a solvent. The reaction of compounds2,3, and4with DMAD or DEAD led to the formation of 4-oxothiozolidine derivatives(4b–c),(3a-c), and(2c-d). The treatment of compounds2,3, and4with 1, 4′-diboromoacetophenone resulted in the formation of thiazole derivatives(2g, 3f, 4f). The treatment of compounds2,3, and4with sulfuric led to the formation of 4H-1,2,4-triazole-3-thiol der

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Aliya, Sireesha B., Venkata Ramana Reddy Ch., and Sarala Devi Ch. "Spectral and equilibrium studies on some new derivatives of 4-amino-5-phenyl-3-mercapto-1,2,4-triazole." Journal of Indian Chemical Society Vol. 85, Sep 2008 (2008): 926–29. https://doi.org/10.5281/zenodo.5820217.

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Department of Chemistry, Nizam College, Osmania University, Hyderabad-500 001, India <em>E-mail:</em> dr_saraladevich@yahoo.com <em>Manuscript received 1 October 2007, revised 3 June 2008, accepted 17 June 2008</em> 4-Amino-5-phenyl-3-mercapto-1,2,4-triazole (APMT), 4-(4'-methoxy)benzylidineamino-5-phenyl-3-mercapto-1,2,4- triazole (PMBPMT), 4-benzylidineamino-5-phenyl-3-mercapto-1,2,4-triazole (BPMT), 4-(2´-hydroxy)benzyhdmeammo-5-phenyl-3-mercapto-1 2,4-triazole (HBPMT) and 4-amino-5-(4' -nitro)phenyl-3-mercapto-1,2,4-triazole (ANPMT) were synthesized and characterized by

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Natalia, Chalenko, Demchenko Anatoly, and Syrova Ganna. "Synthesis of potential antiexudative preparations for 2-((4-amino-5-(furan-2-il)-1,2,4-triazole-(4H)-3-yl)-sulfanyl)-N-acetamide series." ScienceRise: Pharmaceutical Science, no. 3(19) (June 28, 2019): 22–29. https://doi.org/10.15587/2519-4852.2019.171878.

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<strong>Aim.</strong> Conduct the purposeful synthesis of new potential biologically active substances of derivatives of 2 - ((4-amino-5- (furan-2-yl) -1,2,4-triazol (4H) -3-yl) -sulfanyl) -N-acetamides and evaluate their anti-exudative activity on the model of formalin edema in rats. <strong>Materials and methods.</strong> In this work, standard methods of organic synthesis, physical and chemical methods of proofing the structure of synthesized compounds, elemental analysis, <sup>1</sup>H NMR spectroscopy, chromatographic mass spectrometry, and antiexudative activity were studi

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40

Chittimalla, Srinivasulu, Jalapathi Pochampally, Vishnu Thumma, Umapathi Nalla, and Raghavender Matta. "Synthesis, antimicrobial activity and molecular docking study of (e)-4-(4-((3-benzylidene-2-oxoindolin-1-yl) methyl)-1h-1,2,3-triazol-1-yl)benzoic acid derivatives." Research Journal of Chemistry and Environment 27, no. 9 (2023): 39–45. http://dx.doi.org/10.25303/2709rjce039045.

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A series of (E)-1-((1-aryl-1H-1,2,3-triazol-4-yl) methyl)-3-(arylmethylene)indolin-2-ones was synthesised starting from commercially available indolin-2-one by the reaction with aldehydes, propargyl bromide and finally benzoic acid azides. All the synthesized 1,2,3-triazole derivatives structure were characterized by IR, 1HNMR, 13CNMR and mass spectrometry. The synthesized compounds were evaluated for their in vitro antimicrobial activity and their molecular docking studied with comparison of Oseltamivir drug into the active pocket of neuraminidase.

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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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Kuldeep, T. Padhyar, S. Patil Rajendra, and B. Wadwale Navanand. "A brief review on Triazole and its Pharmacological Application." International Journal of Current Science Research and Review 05, no. 01 (2022): 212–25. https://doi.org/10.47191/ijcsrr/V5-i1-25.

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  Abstract : The triazole core is one of the most imperative and well known heterocycles which is composed of nitrogen atom which forms natural products with medicinal claims. Triazole moiety is present as a principal structural component in the drug categories such as antimicrobial, anti-inflammatory, analgesic, antineoplastic, antimalarial, antiviral, antihypertensive, local anaesthetic, antianxiety, anti-Parkinson′s, antidepressant, antioxidant, antihistaminic, antitubercular, antidiabetic etc. The broad and potent activity of triazole and their derivatives has established them a

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Susanta, K. Borthakur, Boruah Paran, and N. Goswami Birendra. "[4+2] Cycloaddition reaction: Synthesis and antifungal activities of 2-substituted 1,2,4-triazolo[3,2-c][1,3,5]thiadiazine-3,3-dioxides." Journal of Indian Chemical Society Vol. 90, Jul 2013 (2013): 1005–8. https://doi.org/10.5281/zenodo.5774794.

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Department of Chemistry, Arya Vidyapeeth College, P.O. Gopinath Nagar, Guwahati-781 016, Assam, India <em>E-mail</em> : skbthakur@yahoo.co.in Medicinal Aromatic and Economic Plant Division, Formerly of Synthetic Organic Chemistry Division, North East Institute of Science and Technology, Jorhat-785 006, Assam, India <em>Manuscript received online 06 August 2012, revised 09 August 2012, accepted 16 August 2012</em> 3-Benzylidineamino-1,2,4-triazole undergoes [4+2] cycloaddition reaction with sulfene resulting in good yield of [1,2,4]-triazolo[3,2-<em>c</em>][1,3,5]-thiadiazine-3,3-dioxide deriva

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44

Süleymanoğlu, Nevin, Reşat Ustabaş, Şahin Direkel, Yelda Bingöl Alpaslan, and Yasemin Ünver. "1,2,4-triazole derivatives with morpholine; DFT study and antileishmanial activity." Canadian Journal of Physics 96, no. 7 (2018): 719–23. http://dx.doi.org/10.1139/cjp-2017-0710.

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1,2,4-triazole derivatives with morpholine; 4-((3-methylthiophene–2-yl)methylenamino)-1-((4-(3-methylthiophene–2-yl)methylene amino)-1-(morpholinomethyl)-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-3-yl)methyl)-3-(thiophene–2-ylmethyl)-1H-1,2,4-triazole-5(4H)-one (compound I) and 1-((1-(morpholinomethyl)–4-(5-nitrothiophene–2-yl)methyleneamino)-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-3-yl)methyl)-4-((5-nitrothiophene–2-yl)methyleneamino)-3-(thiophene–2-ylmethyl)-1H-1,2,4-triazole-5(4H)-one (compound II), were optimized using a density functional theory (DFT) method with 6-311G(d,p) basis set and str

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Khan, Imtiaz, Shahid Hameed, Najim A. Al-Masoudi, Nabeel A. Abdul-Reda, and Jim Simpson. "New triazolothiadiazole and triazolothiadiazine derivatives as kinesin Eg5 and HIV inhibitors: synthesis, QSAR and modeling studies." Zeitschrift für Naturforschung B 70, no. 1 (2015): 47–58. http://dx.doi.org/10.1515/znb-2014-0162.

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AbstractA new series of fused 1,2,4-triazoles, namely 6-aryl-3-(furan-2-yl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles 3a–h and 4a–f as well as 6-aryl-3-(furan-2-yl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines 5a–h, were synthesized by the condensation of 4-amino-5-(furan-2-yl)-4H-1,2,4-triazole-3-thiol (2) with substituted aromatic acids and phenacyl bromides, respectively. The structures of the newly synthesized compounds were established using spectroscopic analysis, while that of 3e was confirmed independently by a single-crystal X-ray structure determination. The compounds were evaluated

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Karpun, Yevhen, Volodymyr Parchenko, Tetiana Fotina, et al. "The investigation of antimicrobial activity of some s-substituted bis-1,2,4-triazole-3-thiones." Pharmacia 68, no. (4) (2021): 797–804. https://doi.org/10.3897/pharmacia.68.e65761.

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New S-substituted 4-alkyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol derivatives have been designed, synthesized and studied their antimicrobial activity on 11 standard Gram-positive and Gram-negative microorganism strains. Their spectral and physicochemical parameters were established using modern comprehensive methods of analysis, including <sup>1</sup>H NMR spectroscopy, GC-MS and elemental analysis.It has been found that compound 2a exhibits strong suppression of 5 test strains (MBC = 15.6 µg/mL). Compound 4a showed moderate inhibition of Salmonella

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Yang, Tingting, Xin Shi, Libing Guo, et al. "Design, synthesis, and antitumor activity of novel paeonol derivatives containing the 1,4-benzoxazinone and 1,2,3-triazole moieties." Journal of Chemical Research 43, no. 7-8 (2019): 241–47. http://dx.doi.org/10.1177/1747519819857479.

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A new series of paeonol derivatives containing the 1,4-benzoxazinone and 1,2,3-triazole moieties were synthesized and evaluated for their cytotoxicity in vitro against human non-small cell lung cancer NCI-H1299 cells and human cervical carcinoma HeLa cells. Among them, compared with that of paeonol, compounds 8-acetyl-4-{[(1-(5-chloro-2-nitrophenyl)-1 H-1,2,3-triazol-4-yl]methyl}-5-methoxy-2 H-1,4-benzoxazin-3(4 H)-one, 8-acetyl-4-[(1-mesityl-1 H-1,2,3-triazol-4-yl)methyl]-5-methoxy-2 H-1,4-benzoxazin-3(4 H)-one, and 8-acetyl-5-methoxy-4-{[(1-(naphthalen-1-yl)-1 H-1,2,3-triazol-4-yl]methyl}-2

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48

Khalifa, Nagy M., Ahmed M. Naglah, Mohamed A. Al-Omara, and Abd El-Galil E. Amr. "Synthesis and Reactions of New Chiral Linear Dipeptide Candidates Using Nalidixic Acid as Starting Material." Zeitschrift für Naturforschung B 69, no. 6 (2014): 728–36. http://dx.doi.org/10.5560/znb.2014-4031.

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A series of dipeptide heterocyclic derivatives 4-15 were synthesized using methyl 2-{[(1-ethyl- 7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridin-3-yl)carbonyl]amino}-3-ethylbutanoate (3) as starting material. Treatment of 3 with L-phenylalanine methyl ester hydrochloride afforded the corresponding dipeptide methyl ester derivative 4, which was treated with hydrazine hydrate to afford the dipeptide acid hydrazide 5. Compound 5 was coupled with aldehyde and acetophenone derivatives to afford the corresponding Schiff bases 6a-f. The hydrazide derivative 5 was reacted with ethyl acetoacetate or acetone

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Unnamatla, M. V. Basavanag, Marco A. García-Eleno, and Erick Cuevas Yáñez. "Ionic Liquid Mediated Ugi/SN2 Cyclization: Synthesis of 1,2,3-Triazole Containing Novel 2,5-Diketopiperazines." Proceedings 41, no. 1 (2019): 75. http://dx.doi.org/10.3390/ecsoc-23-06657.

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The Ugi four-component reaction is versatile multicomponent reaction for generation of complex diversity, herein, we developed a novel methodology by using 4-((1-((tetrahydrofuran-2-yl)methyl)-1H-1,2,3-triazol-4-yl)methoxy)benzaldehyde as one of the components in Ugi 4CR that contains 1,2,3-triazole moiety which is a privileged molecule in medicinal chemistry to obtain Ugi adducts under room temperature ionic liquids as medium of solvent, then followed SN2 pathway cyclization to get triazole containing 2,5-diketopiperazine derivatives in good yield using basic ionic liquids as a catalyst.

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Morshed, MH, MF Islam, MA Yousuf, GMG Hossain, JA Khanam, and MA Salam. "Synthesis and Antimicrobial Screening of Three Triazole Derivatives." Dhaka University Journal of Pharmaceutical Sciences 10, no. 1 (2012): 43–47. http://dx.doi.org/10.3329/dujps.v10i1.10014.

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Due to the medicinal importance of triazole derivatives, the antimicrobial property of three synthesized triazole derivatives were screened in vitro against some Gram positive and Gram negative pathogenic bacteria and some pathogenic fungi. In this study, three compounds 2-(5-mercapto-4-phenyl-4H-[1,2,4] triazole-3-yl]-cyclohexa- 1,5-dienol (S1), 2-[5-mercapto-4-(2-mercapto-phenyl)-4H- [1,2,4] triazole-3-yl]-phenol (S2) and 4-[3-(2-hydroxyphenyl)- 5-mercapto-[1,2,4] triazole-4-yl]-benzene sulfonamide (S3) have been synthesized. The minimum inhibitory concentration (MIC) and the minimum bacteri

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