Relevant bibliographies by topics / 1;2;4-triazole derivatives

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Academic literature on the topic '1;2;4-triazole derivatives'

Author: Grafiati
Published: 4 June 2025
Last updated: 23 June 2025

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

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>&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)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol series, and study some regularities of the &ldquo;structure &ndash; biological activity&rdquo; relationship for the synthesized compounds as well. <strong>Materials and methods.</strong>&nbsp;The subject of the study was new S-substituted 1,2,4-triazoles containing 2-oxopropan-1-yl and 2-aryl-2-oxoethan-1-yl substituents. The antimicrobial activity was studied by double serial dilutions on test cultures of Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), and Candida albicans (ATCC 885-653). <strong>The results</strong>&nbsp;of the biological screening showed that at a concentration of 125 g/mL, all synthesized substances showed activity (MIC &ndash; in the range of 31.25 - 62.5 &mu;g/mL, MBCK - in the range of 62.5&ndash;125 &mu;g/mL) against strains of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans. Variation of substituents on the sulfur atom did not lead to a significant change in antimicrobial and antifungal activities among derivatives of 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl) thio)methyl)-4H-1,2,4-triazole-3-thiols. <strong>Conclusions.</strong>&nbsp;Biological screening data indicate the prospects for the search for new antimicrobial substances among the abovementioned derivatives of 1,2,4-triazoles. The most active compounds were 1-((4-ethyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)propan-2-one and 1-(4-methoxyphenyl)-2-(4-ethyl-5-(((3-(pyridin-4-yl)-1H)-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)ethanone, which showed the most pronounced antimicrobial activity against the Pseudomonas aeruginosa strain (MIC &ndash; 31.25 &mu;g/mL, MBcK - 62.5 &mu;g/mL)
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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)thio)methyl)-4H-1,2,4-triazole-3-thiol series, and study some regularities of the “structure – biological activity” relationship for the synthesized compounds as well.&#x0D; Materials and methods. The subject of the study was new S-substituted 1,2,4-triazoles containing 2-oxopropan-1-yl and 2-aryl-2-oxoethan-1-yl substituents. The antimicrobial activity was studied by double serial dilutions on test cultures of Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), and Candida albicans (ATCC 885-653).&#x0D; The results of the biological screening showed that at a concentration of 125 g/mL, all synthesized substances showed activity (MIC – in the range of 31.25 - 62.5 μg/mL, MBCK - in the range of 62.5–125 μg/mL) against strains of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans. Variation of substituents on the sulfur atom did not lead to a significant change in antimicrobial and antifungal activities among derivatives of 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl) thio)methyl)-4H-1,2,4-triazole-3-thiols.&#x0D; Conclusions. Biological screening data indicate the prospects for the search for new antimicrobial substances among the abovementioned derivatives of 1,2,4-triazoles. The most active compounds were 1-((4-ethyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)propan-2-one and 1-(4-methoxyphenyl)-2-(4-ethyl-5-(((3-(pyridin-4-yl)-1H)-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)ethanone, which showed the most pronounced antimicrobial activity against the Pseudomonas aeruginosa strain (MIC – 31.25 μg/mL, MBcK - 62.5 μg/mL)
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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 dicarboxylic acid hydrazides (a-e). The structures of the newly All the compounds synthesised 6a to 6e were evaluated for antifungal activity against Candida albicans and Aspergillus Niger was carried out and MIC values were determined synthesized compounds were estblished by FT-IR, 1H-NMR and MASS spectral analysis. The compound 6a (n=0) was found to be the most potent antifungal agent. Keywords: 1,2,4-triazole derivatives, antifungal, Candida albicans, Aspergillus Niger
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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-triazole derivatives (4a-b) with 4-mesyl-1-boc-piperidine (5) under basic conditions using sodium hydride, which further on acidic deprotection followed by benzylation reaction furnished dibenzyl N(2)-C-linked triazolyl piperidines (9a-j).
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*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-triazole derivatives, they are well-known and widely used among organic chemists in the process of creating new unique molecules. The gradual, predicted introduction of different substituents into the 1,2,4-triazole derivative molecules leads to the appearance of new types of biological activity, and in some cases, this increases the activity levels already observed. Chemical modification of the compounds by altering substituents around the 1,2,4-triazole fragment fundamentally changes the type of biological activity of the new molecules. Despite the constant criticism of synthetic drugs, their role in healthcare cannot be overestimated. The ability to continuously improve synthetic molecules makes original drugs more effective and keeps them in high demand. The scientific school of Zaporizhzhia State Medical University has synthesized a significant number of 1,2,4-triazole derivatives[7&ndash;11] and developed various methods for their heterocyclization. The current scientific potential of new 1,2,4-triazole derivatives has been analyzed. The new compounds have proven to be promising biologically active agents. The wide possibilities for their application create favorable conditions for further research into new molecules based on 1,2,4-triazole.
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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-tolyloxyacetohydrazide, which is further reacted with ethyl isothiocyanate to produce 2-p-tolyloxythiosemicarbazide. Cyclizing 275 in an alkaline media generates 4-ethyl-5-(p-tolyloxymethyl)-4H-1, 2, 4-triazole-3-thiol. 276 interacts with several alkyl halides in the last stage to create N-ethyl-3, 5-substituted derivatives (278a-h). Infrared (IR), nuclear magnetic resonance (NMR), electron ionization mass spectrometry (EI-MS), and high-resolution electron ionization mass spectrometry (HR-EI-MS) were used to characterize each chemical. This work adds to the expanding area of nitrogen-rich heterocycles by providing fresh triazole derivatives with possible uses in industrial and medical chemistry.
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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 synthesized compounds. all the final synthesized compounds (5–11) were tested for antimicrobial activity. The findings of this study demonstrate the viability of synthesizing vanillic acid combined with a 1, 2, 4-triazole-3-thiol ring derivative, which then reacted with various aldehydes to yield several new Schiff bases derivatives. Finally, the presence of an electron-withdrawing group at the fourth position (p- chloro group) of the aromatic ring improves the antibacterial activity of the derivative of the vanillic acid-triazole conjugate. Compound 8 with para chloro substituted Schiff base derivative showed potent activity when compared to other final derivatives but of no activity toward K. pneumonia.
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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-oxo-1,2,4-triazoles with chloroacetyl chloride in presence of a non-polar solvent like benzene. Elemental analysis, GCMS, IR, and1H NMR confirmed the structures of the newly synthesised compounds. The newly synthesized compounds are also screened for their antibacterial, antifungal and anti-inflammatory activities.
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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 labelled with no carrier added 123I or 125I and purified by high performance liquid chromatography to give isolated radiochemical yields between 6% and 51% and radiochemical purities of &gt;95% in all cases. Among the evaluated compounds, N-(2-diethylamino-ethyl)-2-(4-iodo-[1,2,3]triazol-1-yl)acetamide (7a) and N-(1-benzylpiperidin-4-yl)-2-(4-iodo-1H-1,2,3-triazol-1-yl)acetamide (7d) showed the most promising in vivo data, and their 123I-labelled forms were used in single photon emission computed tomography computed tomography (SPECT–CT) imaging studies. The imaging data showed excellent tumour visualization with a very high signal to noise ratio.
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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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Dissertations / Theses on the topic "1;2;4-triazole derivatives"

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Kitagawa, Kristen. "Studies in the asymmetric reduction of (3s)-3-amino-1-chloro-4-phenyl-2-butanone derivatives." Diss., Georgia Institute of Technology, 2010. http://hdl.handle.net/1853/39464.

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This thesis focuses on the asymmetric reduction of N-protected derivatives of (3S)-3-amino-1-chloro-4-phenyl-2-butanone to their corresponding diastereomeric alcohol products, which are key intermediates in the synthesis of HIV protease inhibitors. Although the stereoselective synthesis of the (S,S) alcohol product is easily achieved, preparing the (R,S) diastereomer is much more challenging. I investigated three diastereoselective reduction processes: 1) Meerwein-Ponndorf-Verley (MPV) reduction, 2) asymmetric transfer hydrogenation, and 3) boron reducing agents. The diastereoselectivity of the MPV reduction still favored the (S,S) product; however, I discovered a significant rate enhancement when the standard catalyst (aluminum isopropoxide) was replaced with aluminum tert-butoxide. Many reaction variables were investigated in the asymmetric transfer hydrogenation reaction and the diastereoselectivity was improved to give a ratio of the desired (R,S) diastereomer to the undesired (S,S) alcohol of 9.5:1. Using chiral oxazaborolidine catalysts, an unprecedented (R,S) to (S,S) ratio of 9.5:1 was achieved. Finally, I investigated the effect of the N-protecting group on the stereoselectivity of the reduction. When the original boc-protecting group was replaced with a phthalimide group, the diastereoselectivity of the MPV reduction was reversed to favor the desired (R,S) product.
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Fowles, A. M. "The preparation and biological activity of some 2-alkylated gibberellin Asub(4) and Asub(1) derivatives." Thesis, University of Bristol, 1986. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.370827.

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Nguyen, Dao. "Design, Synthesis, and Characterization of Novel Hydrophilic Fluorene-Based Derivatives for Bioimaging Applications." Doctoral diss., University of Central Florida, 2009. http://digital.library.ucf.edu/cdm/ref/collection/ETD/id/2842.

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In this work, hydrophilic fluorene-based derivatives that contain ethylene oxide substituents, have been synthesized and characterized for potential use as new fluorophores for bioimaging applications and for fluorescence sensing of heavy metals. Symmetrical and unsymmetrical fluorene derivatives based on structural types of acceptor-pi-acceptor, acceptor-pi-donor, and donor-pi-donor were characterized by TGA, UV-vis absorption, fluorescence emission, lifetime, anisotropy, and two-photon absorption (2PA) cross section. They were found to possess high thermal stability, high photostability, high fluorescence quantum yields, and generally large two-photon absorption cross sections, making them quite suitable for new probes in single-photon absorption and two-photon absorption fluorescence microscopy imaging. Novel hydrophilic fluorene derivatives were synthesized from fluorene in multiple steps employing the metal-catalyzed Heck coupling reaction, the Stille reaction, the Sonogashira reaction, the Ullmann condensation reaction, and "click" chemistry. To increase the hydrophilicity of the new compounds, ethylene oxide substituents were utilized for to impart water solubility. An alternative alkylation methodology using ethyleneoxy tosylates was introduced for the synthesis of ethylene oxide-containing fluorene derivatives. Several of these hydrophilic derivatives were incubated into various cell lines as new probes for both conventional and two-photon absorption fluorescence bioimaging. These compounds were biocompatible, exhibiting low cytotoxicity as determined by cell viability studies, and displayed colocalization for selected cellular organelles. In addition, hydrophilic bis(1,2,3-triazolyl)fluorene derivatives were found to exhibit sensitive fluorescence responses in the presence of certain heavy metal, and were selective for sensing zinc and mercury over other a number of other metal ions relevant to living cells or other biological environments. The UV-vis absorption and fluorescence emission spectra of the complexes exhibited a blue-shifted absorption and emission for selective metal chelation upon binding to zinc and mercury(II) ions, resulting in an approximately two-fold enhanced fluorescence response. Fluorescence titration studies revealed that the complexes of 1:2 and 1:3 ligand to metal formed with binding constant values of 108 and 1014 for zinc and mercury ions, respectively. Finally, preliminary experiments were performed to explore the possibility of employing select hydrophilic fluorene-based derivatives in the synthesis of hydrophilic fluorescent gold nanoparticles. Although results are very preliminary, the aim is to use such materials for other biomedical applications, such as surface enhanced scattering resonance and noninvasive photothermal therapy to diagnose and to treat cancers. Thus, this research had led to the discovery of alternative methodologies for synthesis of hydrophilic fluorene derivatives by alkylation with alkyl tosylates and synthesis of hydrophilic fluorescent molecule capped gold nanoparticles. Furthermore, several novel hydrophilic fluorene-based derivatives were synthesized and characterized for their linear and nonlinear photophysical properties, and are now available for further examination of their bioimaging and sensing applications.<br>Ph.D.<br>Department of Chemistry<br>Sciences<br>Chemistry PhD
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Osazee, Joseph Osamudiamen. "Molecular Docking, Synthesis and Evaluation of Pyrrolo[2,1-c][1,4]benzodiazepines Derivatives as Non-β-lactam β-lactamases Inhibitors". Digital Commons @ East Tennessee State University, 2016. https://dc.etsu.edu/etd/3082.

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Our research aim was to design, synthesize, and study the competitive enzyme inhibition kinetics of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives as potential non-²-lactam ²-lactamase inhibitors. All compounds (1-13) passed the Lipinski’s rule of 5 test and were docked into the active site of TEM-1 ²-lactamase. PBD derivatives 1-7 were synthesized in high yields and tested for their potency against TEM-1 and P99 ²-lactamases. Kinetic data showed that compounds 1, 4, 5, and 7 possessed inhibitory activity against TEM-1 ranging from 4-34 %. Docking results revealed significant interactive spanning of the active site of TEM-1 by PBDs. The limited inhibitory activity of the compounds, 1-7 could be attributed to the lack of solubility and bulky nature of the molecules, thus limiting the optimal ligand-enzyme interactions. 1,2,4- Oxadiazolinones (8-13) were further synthesized to reduce the steric hindrance of the PBD scaffolds while promoting the electrophilicity of the potentially active lactam and also evaluated for potency.
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KROBER, JONAS. "Materiaux moleculaires a transition de spin pour l'affichage : derives du fe (ii) -1, 2, 4 - triazole." Paris 11, 1994. http://www.theses.fr/1994PA112091.

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Ce travail de these est consacre a l'etude du phenomene de transition du spin (ts) dans les composes a base moleculaire contenant des ions fe #i#i entoures de derives 1,2,4-triazoles. La ts se manifeste dans ces composes par un passage thermoinduit de l'etat fondamental bas-spin diamagnetique (bs ou s=0) vers un etat legerement excite paramagnetique haut-spin (hs ou s=2). Ce passage est accompagne d'un effet thermochrome important du rouge vers le blanc. Un des buts principaux etait l'utilisation de cet effet thermochrome afin de realiser des dispositifs servant au stockage de l'information, le premier objectif etant des dispositifs d'affichage. A cette fin, les composes doivent presenter une large hysteresis thermique, de l'ordre de plusieurs dizaines de kelvin et il est crucial que ces effets se manifestent aussi pres que possible de la temperature (t) ambiante. Un premier candidat potentiel etait le compose fe(htrz)#2(trz)bf#4 ou htrz represente le 1,2,4-1h-triazole et trz la base correspondante. Ce compose presente une hysteresis tres large, d'environ 50 k, avec des ts tres abruptes (moins que 5 k). Les proprietes de la ts dependent beaucoup de la preparation du compose. Le compose non deprotone fe(htrz)#3(bf#4)#2 presente en plus d'une hysteresis proche de l'ambiante une transition de phase a 150c qui deplace les t de la ts reversiblement en dessous de l'ambiante. Potentiellement ce compose permet l'acces a des hysteresis de 100 k. L'ajustement des t de la ts par dopage partiel du ligand est etudie pour le compose fe(htrz)#3#-#3#(nh#2trz)#3#(clo#4)#2 (nh#2trz=4-amino-1,2,4-triazole) presentant pour =0,05 une boucle d'hysteresis centree autour de la t ambiante. Le remplacement de la substitution de bf#4 par br#- dans le compose fe(nh#2trz)#3(bf#4)#2 conduit a un deplacement de la t de la ts autour de l'ambiante et celle-ci devient beaucoup plus abrupte. Tous ces composes ont des structures polymeriques. Ils se presentent sans doute sous forme de chaines. Afin de comprendre les proprietes physiques de ces composes qui sont etroitement liees a leurs structures, nous avons etudie par diffraction des rayons x la structure de deux composes, zntrzc1, presentant une structure lamellaire et le compose trinucleaire fe#3(me#2ntrz)#6(h#2o)#6(clo#4)#6 (me#2ntrz=4-dimethylamino-1,2,4-triazole). Certains des composes decrits dans cette these ont conduit a des dispositifs deja tres proches du marche. Cette composante de notre travail a ete menee a bien en collaboration avec un partenaire industriel
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El, Haj Brahim Ichrak. "Préparation stéréosélective de 2-alcynyldiols-1,3 ou 2-alcynylaminoalcools-1,3 : synthèse des hétérocycles condensés issus du 2- aminobenzonitrile." Electronic Thesis or Diss., Sorbonne université, 2023. https://accesdistant.sorbonne-universite.fr/login?url=https://theses-intra.sorbonne-universite.fr/2023SORUS495.pdf.

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Cette thèse s'est orientée autour de deux axes de recherche distincts. En premier lieu, nous avons exploré la synthèse des 4-hydroxy-1-boryl-1-allenylsilanes, en adoptant une approche innovante à partir d'époxydes acétyléniques et du (triéthylsilyl)pinacolborane. Cette méthode a permis une préparation stéréosélective et stéréospécifique d'allénylboranes, suivant un mécanisme SNi anti. De plus, l'utilisation de ces 4-hydroxy-1-boryl-1-allenylsilanes pour la propargylation des aldéhydes a conduit, de manière stéréosélective, aux 2-alcynyldiols-1,3. Un état de transition impliquant une structure à six chaînons fermés a été proposé pour cette transformation, suggérant un mécanisme SE2’. L'ampleur et les limitations de ces deux processus ont été rigoureusement examinées. Ensuite, le second aspect de cette thèse a concerné la synthèse de composés hétérocycliques à partir du 2-aminobenzonitrile, en mettant l'accent sur le 1,2,4-triazole. Nous avons par la suite élaboré des dimères et étudié leur réactivité envers des électrophiles, tels que le hexaméthylphosphoramide, avec l'objectif de créer des dérivés de diazaphorine. À l'heure actuelle, une analyse est en cours pour évaluer les propriétés antioxydantes des molécules récemment synthétisées, en particulier des dimères iminiques et phosphoazotés<br>This thesis revolved around two distinct research avenues. Firstly, we delved into the synthesis of 4-hydroxy-1-boryl-1-allenylsilanes, adopting an innovative approach using acetylenic epoxide and silylborane. This method enabled a stereoselective and stereospecific preparation of allenylboranes, following an SNi anti mechanism. Moreover, we employed these allenes for the propargylation of aldehydes, which led to the stereoselective formation of the corresponding 2-alkynyl-1,3-diols. A transition state involving a closed six-membered ring structure was proposed for this transformation, suggesting an SE2' mechanism. The scope and limitations of these processes were meticulously assessed. Subsequently, the second focus of the thesis pertained to the synthesis of heterocyclic compounds starting from 2-aminobenzonitrile, with a particular emphasis on the 1,2,4-triazole. Following this, we synthesized dimers and investigated their reactivity towards electrophiles, such as hexamethylphosphoramide, aiming to generate diazaphorine derivatives. As of now, an evaluation is underway to gauge the antioxidant properties of the newly synthesized molecules, especially the iminic and phosphoazo dimers
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chaudhary, Arpana S. "Inhibitors of SecA as Potential Antimicrobial Agents." Digital Archive @ GSU, 2013. http://digitalarchive.gsu.edu/chemistry_diss/77.

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Protein translocation is essential for bacterial survival and the most important translocation mechanism in bacteria is the secretion (Sec) pathway. Thus targeting Sec pathway is a promising strategy for developing novel antibacterial therapeutics. We report the design, syntheses, mechanistic studies and structure-activity relationship studies using HQSAR and 3-D QSAR Topomer CoMFA analyses of 4-oxo-5-cyano thiouracil derivatives. In summary, introduction of polar group such as –N3 and linker groups such as –CH2-O- enhanced the potency as well as logP and logS several fold. We also report the discovery, optimization and structure-activity relationship study of 1,2,4-triazole containing pyrimidines as novel, highly potent antimicrobial agents. A number of inhibitors have been found to inhibit microbial growth at high nanomolar concentrations.
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Ciccolini, Cecilia. "Synthesis of Mono and Poly-Heterocycles starting from 1,2-Diaza-1,3-Dienes (or precursors) as Building Blocks." Doctoral thesis, Urbino, 2020. http://hdl.handle.net/11576/2674162.

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Ju, Chen Hui, and 陳慧茹. "The study on the synthesis of 1, 2-dialkoxycalix[4]arenes via benzoate derivatives." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/61630872816837131132.

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碩士<br>中國文化大學<br>應用化學研究所<br>97<br>Abstract Calixarenes, which are cyclic oligomers of p-substituted phenols and formaldehyde , are able to include small organic molecules or metal ions within the molecular cavities to form“ host-guest”complexes. These phenomena have been proposed in the applications of micro-analysis, ion separation, and enzyme-mimic studies. The main purpose of this thesis is to study the synthesis of calix[4]arene 1,2-dialkyl ethers . In the basic conditions, p-tert-butylphenol were polymerized with formaldehyde to form a yellowish precursor. Refluxing of this precursor in diphenyl ether yielded the p-tert-butylcalix[4]arene (1). The AlCl3 catalyzed reverse Friedel-Crafts reaction were then applied to remove the p-tert-butyl groups and gave parent calix[4]arene (6). In our earlier studies on the preparation of calix[4]arene ethers, we have noticed that in the presence of sodium methoxide , the monoalkylated calix[4]arenes can be prepared by refluxing calix[4]arene with alkyl halides in CH3CN. Five different alkyl halides, iodoethane, 1-iodopropane, 1-iodobutane, allyl bromide, and benzyl bromide, were applied in this synthetic procedure. Esterification of those monoalkylated calix[4]arenes 29-33 with an excess of benzoyl chloride in pyridine produced the corresponding 25-alkoxy-27-benzoyloxy-26,28-dihydroxycalix[4]arenes 34-38 and 25,26-dibenzoyloxy-27-alkoxy-28-hydroxycalix[4]arenes 39-43 . Products 34-38 were treated with NaH and alkyl halides in CH3CN to introduce the second alkyl ether linkage and yielded 25,26-dialkoxy -27-benzoyloxy-28-hydroxycalix[4]arenes 44、45. The removal of benzoate moieties in basic conditions would yield the corresponding final products,1,2-dialkoxycalix[4]arenes 46、47. All the new products which were produced in this thesis were characterized by 1H-NMR, 13C-NMR, COSY, and FAB-MS. The synthetic procedure for 1,2-dialkoxycalix[4]arenes were also discussed in this thesis.
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Wang, Yu-Yun, and 王雨筠. "The Synthesis of Calix[4]arenes with (1) Distal Anthryl-triazoles and Acid Derivatives (2) Distal Bis-Pyrenyl-ester-triazoles for Metal Ion Sensing Studies." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/18427518349799494126.

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碩士<br>國立交通大學<br>應用化學系所<br>97<br>(1) The Synthesis of calix[4]arenes with Distal Anthryl-triazoles and Acid Derivatives for Metal ion Sensing Studies. We used the Click Chemistry to modify the lower rim of calix[4]arenes with a triazole cationic binding site, and an anthracene as a fluorophore. After we incorporating a second acid derivatives group into 5a, compounds 6a�{9a were obtained as fluoroionophores for metal ions. Compounds 5a�{9a and control compound 10a showed fluorescence quenching toward Cu2+, Hg2+, and Cr3+ ions. Besides that, 6a also showed a slight fluorescence quenching toward Pb2+ and Mn2+ ions; 8a showed fluorescence enhancement toward Ba2+, Ca2+, Cd2+, Li+, Mg2+, Pb2+ and Zn2+ ions; 9a showed fluorescence enhancement toward Ag+ and Cd2+. We inferred that the functional groups (amide and thioamide) of 8a and 9a might donate electrons to the anthryl group via PET mechanism, thus the fluorescence of anthryl group was quenched. When the functional groups of 8a and 9a bind with metal ions, the metal ions may inhibit the PET mechanism, and therefore enhance the fluorescence. Possible binding modes of these metal complexes were proposed based on 1H NMR titration experiments. (2) The Synthesis of calix[4]arenes with Distal Pyrenyl-ester-triazoles for Metal ion Sensing Studies. The lower-rim of calix[4]arenes was modified with triazoles as the cationic binding sites, and pyrenes as the fluorophores. Mono-substituted compound 15, bis-substituted compound 16, phenol protected compound 18 and control compound 14 were synthesized. Both 14 and 15 showed fluorescence quenching toward Cu2+, Hg2+ and Cr3+ ions. 16 showed both monomer and excimer fluorescence quenching toward Cu2+and Cr3+, but showed monomer enhancement and excimer quenching toward Hg2+. Compound 18 showed monomer enhancement and excimer quenching toward Ag+ and Zn2+ besides Cu2+, Hg2+ and Cr3+ ions. Note that the complex of 18˙Cu2+ formed a static excimer. We used 1H NMR titration experiment to determine possible binding modes of these metal complexes and proved that the hydroxyl group of 16 proceeded oxidation-reduction with Cu2+.
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Books on the topic "1;2;4-triazole derivatives"

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Pettersson-Fasth, Helena. Preparation and functionalization of 4-(p-toluenesulfonamido)-2-alken-1-ol derivatives, and their use in alkaloid synthesis. Acta Universitatis Upsaliensis, 1994.

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McKinlay Gardner, R. J., and David J. Amor. Autosomal Reciprocal Translocations. Edited by R. J. McKinlay Gardner and David J. Amor. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780199329007.003.0005.

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This chapter reviews in detail the question of carriers of autosomal reciprocal translocations and the genetic risks implied for potential offspring of theirs. Examples are offered of the various possibilities due to malsegregation in gametes of theirs: adjacent-1, adjacent-2, 3:1, and the (very rare) 4:0 malsegregation. The chapter provides advice on determining the most likely modes of segregation, according to the different forms of translocation (length of centric segment, length of translocated segment, sizes of derivative chromosomes). The chapter discusses the practical problem of the apparently balanced translocation but which is associated with phenotypic abnormality. Associations with infertility are noted.
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Bardin, Thomas, and Tilman Drüeke. Renal osteodystrophy. Oxford University Press, 2013. http://dx.doi.org/10.1093/med/9780199642489.003.0149.

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Renal osteodystrophy (ROD) is a term that encompasses the various consequences of chronic kidney disease (CKD) for the bone. It has been divided into several entities based on bone histomorphometry observations. ROD is accompanied by several abnormalities of mineral metabolism: abnormal levels of serum calcium, phosphorus, parathyroid hormone (PTH), vitamin D metabolites, alkaline phosphatases, fibroblast growth factor-23 (FGF-23) and klotho, which all have been identified as cardiovascular risk factors in patients with CKD. ROD can presently be schematically divided into three main types by histology: (1) osteitis fibrosa as the bony expression of secondary hyperparathyroidism (sHP), which is a high bone turnover disease developing early in CKD; (2) adynamic bone disease (ABD), the most frequent type of ROD in dialysis patients, which is at present most often observed in the absence of aluminium intoxication and develops mainly as a result of excessive PTH suppression; and (3) mixed ROD, a combination of osteitis fibrosa and osteomalacia whose prevalence has decreased in the last decade. Laboratory features include increased serum levels of PTH and bone turnover markers such as total and bone alkaline phosphatases, osteocalcin, and several products of type I collagen metabolism products. Serum phosphorus is increased only in CKD stages 4-5. Serum calcium levels are variable. They may be low initially, but hypercalcaemia develops in case of severe sHP. Serum 25-OH-vitamin D (25OHD) levels are generally below 30 ng/mL, indicating vitamin D insufficiency or deficiency. The international KDIGO guideline recommends serum PTH levels to be maintained in the range of approximately 2-9 times the upper normal normal limit of the assay and to intervene only in case of significant changes in PTH levels. It is generally recommended that calcium intake should be up to 2 g per day including intake with food and administration of calcium supplements or calcium-containing phosphate binders. Reduction of serum phosphorus towards the normal range in patients with endstage kidney failure is a major objective. Once sHP has developed, active vitamin D derivatives such as alfacalcidol or calcitriol are indicated in order to halt its progression.
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Book chapters on the topic "1;2;4-triazole derivatives"

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Emandi, A., M. Calinescu, S. Ioachim, R. Georgescu, and I. Serban. "Synthesis and Characterization of the 2:1 Copper(II) Complexes With 4-Arylazo-Pyrazol-5-One Derivatives." In Multiphoton and Light Driven Multielectron Processes in Organics: New Phenomena, Materials and Applications. Springer Netherlands, 2000. http://dx.doi.org/10.1007/978-94-011-4056-0_36.

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Lv, Jian, Lei Lv, Xiaomin Zhang, et al. "Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent 2-benzyl-3, 4-dihydroisoquinolin-1(2H)-one and Its Derivatives." In Proceedings of the 2012 International Conference on Applied Biotechnology (ICAB 2012). Springer Berlin Heidelberg, 2013. http://dx.doi.org/10.1007/978-3-642-37922-2_83.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of one dimensional chain compound catena-poly[μ-4, 4′-bis-1, 2, 4-triazole-N1N1]aquabis (4, 4′ -bis-1, 2, 4-triazole-N1)(thiocyanato-N)manganese(II) thiocyanato]." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-49202-4_588.

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Grikina, O. E., L. S. Khaikin, and M. Alcolea Palafox. "Joint Use of AB Initio Calculations, Vibrational Spectroscopy, Electron Diffraction, and Microwave Data in the Investigation of the Structure and Intramolecular Dynamics of 1, 3, 2-Dioxaphospholene and its 2-Chloro- and 2-Chloro-4, 5-Dimethyl- Derivatives." In Spectroscopy of Biological Molecules: Modern Trends. Springer Netherlands, 1997. http://dx.doi.org/10.1007/978-94-011-5622-6_244.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of copper(II) chloride complex with 1, 2, 4-triazole." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-49202-4_51.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of copper(II) bromide complex with 1, 2, 4-triazole." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-49202-4_52.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of copper(II) chloride complex with 1, 2, 4-triazole." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-49202-4_53.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of copper(II) bromide complex with 1, 2, 4-triazole." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-49202-4_54.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of nickel(II) bromide complex with 1, 2, 4-triazole." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2015. http://dx.doi.org/10.1007/978-3-662-45972-0_579.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of iron(II) chloride complex with 1, 2, 4-triazole." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2015. http://dx.doi.org/10.1007/978-3-662-45972-0_356.

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Conference papers on the topic "1;2;4-triazole derivatives"

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Marliyana, Soerya Dewi, Maulidan Firdaus, Muhamad Widyo Wartono, Diana Inas Utami, and Uly Wulan Apriani. "Evaluation of the Antibacterial Activity of Pinostrobin Derivative Compounds from Ethylation and Allylation Reactions." In 8th International Conference on Advanced Material for Better Future. Trans Tech Publications Ltd, 2025. https://doi.org/10.4028/p-s3ucax.

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Temu Kunci (Kaempferia pandurata Roxb.) is one of the plants from the Zingiberaceae family that contains secondary metabolites derived from flavonoids. Studies on the bioactivity of flavonoid compounds from this species have shown various biological activities such as antibacterial, antioxidant, antiviral, antitumor, antipyretic, anti-inflammatory, analgesic, and insecticidal properties. Pinostrobin (5-hydroxy-7-methoxy flavanone) (1) is the major flavonoid found in the rhizomes of this plant and has been successfully derivatized through ethylation and allylation reactions. Two compounds were obtained from the ethylation reaction, namely 5-ethoxy-7-methoxy flavanone (2) and 4'-ethoxy-6'-methoxy chalcone (3), while from the allylation reaction, 5-allyloxy-7-methoxy flavanone (4) and 6-allyl-7-methoxy flavanone (5) were obtained. Compounds 2, 3, 4, and 5 were tested for their antibacterial activity against the Gram-positive bacterium Staphylococcus aureus ATCC 25923 and the Gram-negative bacterium Escherichia coli ATCC 25922 using the agar diffusion method. The results of the inhibition zone measurements showed that compounds 2, 3, 4, and 5 were not active against S. aureus ATCC 25923 and E. coli ATCC 25922.
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Eliwi, Amjad Gali, Zainab Zuhair Mohammad Ali, Fouad A. AL-Saady, Shaemaa Hadi Abdulsada, and Abdul Jabar Khlaf Atia. "Synthesis and acetyl cholinesterase inhibitory activity of new oxazole, 1, 2, 4 - triazole derivatives bearing carbamazepine as nucleus." In 2ND INTERNATIONAL CONFERENCE ON MATERIALS ENGINEERING & SCIENCE (IConMEAS 2019). AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0000455.

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Raposo, M., Ana Sampaio, and G. Kirsch. "Synthesis of 1-amino-4-(2´-thienyl)phthalazine Derivatives." In The 8th International Electronic Conference on Synthetic Organic Chemistry. MDPI, 2004. http://dx.doi.org/10.3390/ecsoc-8-01948.

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Bilan, Dmitri, Sergiu Cojocari, Natalia Sucman, Eughenia Stingaci, and Fliur Macaev. "Transforming the five-membered ring d in a pregnenolone derivative into a six-membered ring through skeletal rearrangement." In Scientific seminar with international participation "New frontiers in natural product chemistry". Institute of Chemistry, Republic of Moldova, 2023. http://dx.doi.org/10.19261/nfnpc.2023.ab22.

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In pursuit of obtaining steroid derivatives containing a triazole moiety in their structure, a series of reactions was conducted (Figure 1). In these reactions, an intermediate compound was the corresponding azide 3, which was subsequently involved in a reaction with the required alkyne to form a 1,2,3-triazole. In click chemistry reactions, it is well-known that catalysts are one-valent copper salts, which can be generated in situ from copper(II) salts. However, the NMR spectra of the main product, isolated from the reaction mass, did not match the expected results.Figure 1. The procedure for synthesizing azides 3 and 4 Upon analyzing the collected data from 1H, 13C, 15N, HSQC, HMBC, and DEPT spectra, it was concluded that under these conditions, a skeletal rearrangement occurs, where the fivemembered ring D expands to a six-membered one, forming a new compound. To confirm this hypothesis, the starting compound 3 was mixed under similar conditions without the addition of a reagent. As a result, the same compound was isolated, and its spectral data corresponded to the structure of 5, which was confirmed through X-ray structural analysis too.Figure 2. The mechanism of the skeletal rearrangement The mechanism of the skeletal rearrangement of steroid derivatives in the presence of copper(I) ions is presented in Figure 2.
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Quintela, J., M. Fernández, V. Ojea, M. Ruiz, S. Conde, and A. Díaz. "Stereoselective Synthesis of 2-Amino-4-phosphono-4-pentenoic Acid Derivatives (AP4 Analogues)." In The 1st International Electronic Conference on Synthetic Organic Chemistry. MDPI, 1997. http://dx.doi.org/10.3390/ecsoc-1-02021.

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Ghodke, Mangesh, Suvarna Wagh, Anna Pratima Nikalje, and Julio Seijas Vázquez. "Ultrasound assisted synthesis of 2, 4-substituted 1, 5- benzothiazepine derivatives." In The 23rd International Electronic Conference on Synthetic Organic Chemistry. MDPI, 2019. http://dx.doi.org/10.3390/ecsoc-23-06704.

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Ruiz, María, Vicente Ojea, M. Fernández, Susanna Conde, Aniana Díaz, and José Quintela. "Stereoselective Synthesis of 2-Amino-2-methyl-4-phosphonobutanoic Acid Derivatives (MAP4 Analogues)." In The 1st International Electronic Conference on Synthetic Organic Chemistry. MDPI, 1997. http://dx.doi.org/10.3390/ecsoc-1-02020.

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Guliyeva, Lala, Muhammed Trawally, Kübra Demir-Yazıcı, Kerem Kaya, Atilla Akdemir, and Özlen Güzel-Akdemir. "Thione or Thiol: Sructural Confirmation of (E)-2-(1-(4-cyanophenyl)ethylidene)-N-(2-fluoro-4-sulfamoylphenyl)hydrazine-1-Carbothioamide and Carbonic Anhydrase Inhibition Studies." In 8th International Students Science Congress. ULUSLARARASI ÖĞRENCİ DERNEKLERİ FEDERASYONU (UDEF), 2024. https://doi.org/10.52460/issc.2024.060.

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Thiosemicarbazones are Schiff bases formed by condensing an aldehyde or ketone with thiosemicarbazide derivatives. TSCs exhibit various biological activities and act as precursors for key scaffolds, with keto-enol tautomerism commonly resulting in thione or thiol forms. This study focuses on synthesizing and confirming the structure of compound 1, (E)-2-(1-(4-cyanophenyl)ethylidene)-N-(2-fluoro-4-sulfamoylphenyl)hydrazine-1-carbothioamide, through a condensation reaction in methanol. Both theoretical and experimental IR and X-ray studies confirm the presence of the thione form and E isomerism. Compound 1 showed inhibitory activity against four human carbonic anhydrase isoforms (hCA I, II, IX, XII) with Ki values of 36.0, 5.7, 29.5, and 7.0 nM, respectively.
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Nikhila, G. R., S. R. Batakurki, and B. C. Yallur. "Synthesis, characterization and antioxidant studies of benzo[4, 5]imidazo[2, 1-b]thiazole derivatives." In PROCEEDINGS OF INTERNATIONAL CONFERENCE ON ADVANCES IN MATERIALS RESEARCH (ICAMR - 2019). AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0023101.

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Živković, Marijana B., Srđan J. Tufegdžić, Sandra B. Šegan, Neda O. Đorđević, and Dušan Sladić. "IN SILICO DRUG-LIKENESS OF STEROIDAL THIAZOLIDIN-4-ONES." In 8th Workshop Food and Drug Safety and Qualit. Vinča Institute of Nuclear Sciences - National Institute of the Republic of Serbia, 2024. http://dx.doi.org/10.46793/8fdsq.pc7mz.

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In silico assessment of drug-likeness of 15 steroidal mono- and bis-thiazolidinones was performed. Androstrane (1−5) and progesterone types (6) mono-derivatives had no violations of Lipinski’s rule of five, while bis-derivatives had slightly higher molecular masses than 500 Da, and cholestane derivatives (8−9) showed high lipophilicity and Caco-2 permeability. All examined compounds showed great intestinal absorption potential.
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Reports on the topic "1;2;4-triazole derivatives"

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Ruangpornvisuti, Vithaya. Acidity and basicity investigation for novel derivative of salen and stabilities of their complexes with metal cations : research report. Chulalongkorn University, 2002. https://doi.org/10.58837/chula.res.2002.32.

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Salen derivative, 4 was synthesized and studied for determination of its protonation constants by potentiometric titration. The protonation constants at 25 degree Celsius in 0.1 and 0.5 M KNO[subscript 3] are log K[subscript 1]=10.06, log K[subscript 2]=7.96, log K[subscript 3] = 7.12, log K[subscript 4]= 3.28 and log K[subscript 1]=10.48, log K[subscript 2]=7.99, log K[subscript 3] = 4.71, log K[subscript 4] =2.77, respectively. Complexation for the 4 complexes with Ni(II), Cu(II) and Zn(II) in 0.01 M Bu[subscript 4]NCF[subscript 3]SO[subscript 3] in MeOH were determined by UV-VIS spectrometric titration. The Stability constants, in terms of log[beta] [subscript 11], the 4 complexes with Ni(II), Cu(II) and Zn(II) are 3.80, 4.28 and 4.37, respectively.
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Gurevitz, Michael, William A. Catterall, and Dalia Gordon. Learning from Nature How to Design Anti-insect Selective Pesticides - Clarification of the Interacting Face between Insecticidal Toxins and their Na-channel Receptors. United States Department of Agriculture, 2010. http://dx.doi.org/10.32747/2010.7697101.bard.

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Structural details on the interacting faces of toxins and sodium channels (Navs), and particularly identification of elements that confer specificity for insects, are difficult to approach and require suitable experimental systems. Therefore, natural toxins capable of differential recognition of insect and mammalian Navs are valuable leads for design of selective compounds in insect control. We have characterized several scorpion toxins that vary in preference for insect and mammalian Navs, and identified residues important for their action. However, despite many efforts worldwide, only little is known about the receptor sites of these toxins, and particularly on differences between these sites on insect and mammalian Navs. Another problem arises from the massive overuse of chemical insecticides, which increases resistance buildup among various insect pests. A possible solution to this problem is to combine different insecticidal compounds, especially those that provide synergic effects. Our recent finding that combinations of insecticidal receptor site-3 toxins (sea anemone and scorpion alpha) with scorpion beta toxins or their truncated derivatives are synergic in toxicity to insects is therefore timely and strongly supports this approach. Our ability to produce toxins and various Navs in recombinant forms, enable thorough analysis and structural manipulations of both toxins and receptors. On this basis we propose to (1) restrict by mutagenesis the activity of insecticidal scorpion -toxins and sea anemone toxins to insects, and clarify the molecular basis of their synergic toxicity with antiinsect selective -toxins; (2) identify Nav elements that interact with scorpion alpha and sea anemone toxins and those that determine toxin selectivity to insects; (3) determine toxin-channel pairwise side-chain interactions by thermodynamic mutant cycle analysis using our large collection of mutant -toxins and Nav mutants identified in aim 2; (4) clarify the mode of interaction of truncated -toxins with insect Navs, and elucidate how they enhance the activity of insecticidal site-3 toxins. This research may lead to rational design of novel anti-insect peptidomimetics with minimal impact on human health and the environment, and will establish the grounds for a new strategy in insect pest control, whereby a combination of allosterically interacting compounds increase insecticidal action and reduce risks of resistance buildup.
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Kiss, F., and M. Coyle. First vertical derivative of the magnetic field, aeromagnetic survey of the south Rae Craton, NTS 75 B/1, 2, 3, 4, 5, 6, 7, 8, Northwest Territories. Natural Resources Canada/ESS/Scientific and Technical Publishing Services, 2012. http://dx.doi.org/10.4095/291802.

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Kiss, F., and M. Coyle. First vertical derivative of the magnetic field, aeromagnetic survey of the south Rae Craton, NTS 75 H/1, 2, 3, 4, 5, 6, 7, 8, Northwest Territories. Natural Resources Canada/ESS/Scientific and Technical Publishing Services, 2012. http://dx.doi.org/10.4095/291808.

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Kiss, F., and M. Coyle. First vertical derivative of the magnetic field, aeromagnetic survey of the south Rae Craton, NTS 75 G/1, 2, 8 and parts of G/3, 4, 6, 7, Northwest Territories. Natural Resources Canada/ESS/Scientific and Technical Publishing Services, 2012. http://dx.doi.org/10.4095/291806.

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Kiss, F., and O. Boulanger. First vertical derivative of the magnetic field, aeromagnetic survey of the Frances Lake area, Yukon, NTS 105-G/16 and parts of 105-G/15, H/13, 14, I/4, J/1, 2. Natural Resources Canada/ESS/Scientific and Technical Publishing Services, 2016. http://dx.doi.org/10.4095/298685.

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Kiss, F., and M. Coyle. First vertical derivative of the magnetic field, aeromagnetic survey of the Dawson area, NTS 116-B/4, 116-B/5, 116-C/1, 116-C/2, 116-C/7 and 116-C/8, Yukon. Natural Resources Canada/ESS/Scientific and Technical Publishing Services, 2014. http://dx.doi.org/10.4095/295110.

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Coyle, M., O. Boulanger, V. Tschirhart, and F. Kiss. First vertical derivative of the magnetic field, aeromagnetic survey of the northern Boothia Peninsula II, Nunavut, NTS 57-F/7, 8, 9, 10 and parts of 57-F/1, 2, E/4, 5, 12. Natural Resources Canada/ESS/Scientific and Technical Publishing Services, 2016. http://dx.doi.org/10.4095/299459.

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Payment Systems Report - June of 2020. Banco de la República de Colombia, 2021. http://dx.doi.org/10.32468/rept-sist-pag.eng.2020.

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Abstract:
With its annual Payment Systems Report, Banco de la República offers a complete overview of the infrastructure of Colombia’s financial market. Each edition of the report has four objectives: 1) to publicize a consolidated account of how the figures for payment infrastructures have evolved with respect to both financial assets and goods and services; 2) to summarize the issues that are being debated internationally and are of interest to the industry that provides payment clearing and settlement services; 3) to offer the public an explanation of the ideas and concepts behind retail-value payment processes and the trends in retail payments within the circuit of individuals and companies; and 4) to familiarize the public, the industry, and all other financial authorities with the methodological progress that has been achieved through applied research to analyze the stability of payment systems. This edition introduces changes that have been made in the structure of the report, which are intended to make it easier and more enjoyable to read. The initial sections in this edition, which is the eleventh, contain an analysis of the statistics on the evolution and performance of financial market infrastructures. These are understood as multilateral systems wherein the participating entities clear, settle and register payments, securities, derivatives and other financial assets. The large-value payment system (CUD) saw less momentum in 2019 than it did the year before, mainly because of a decline in the amount of secondary market operations for government bonds, both in cash and sell/buy-backs, which was offset by an increase in operations with collective investment funds (CIFs) and Banco de la República’s operations to increase the money supply (repos). Consequently, the Central Securities Depository (DCV) registered less activity, due to fewer negotiations on the secondary market for public debt. This trend was also observed in the private debt market, as evidenced by the decline in the average amounts cleared and settled through the Central Securities Depository of Colombia (Deceval) and in the value of operations with financial derivatives cleared and settled through the Central Counterparty of Colombia (CRCC). Section three offers a comprehensive look at the market for retail-value payments; that is, transactions made by individuals and companies. During 2019, electronic transfers increased, and payments made with debit and credit cards continued to trend upward. In contrast, payments by check continued to decline, although the average daily value was almost four times the value of debit and credit card purchases. The same section contains the results of the fourth survey on how the use of retail-value payment instruments (for usual payments) is perceived. Conducted at the end of 2019, the main purpose of the survey was to identify the availability of these payment instruments, the public’s preferences for them, and their acceptance by merchants. It is worth noting that cash continues to be the instrument most used by the population for usual monthly payments (88.1% with respect to the number of payments and 87.4% in value). However, its use in terms of value has declined, having registered 89.6% in the 2017 survey. In turn, the level of acceptance by merchants of payment instruments other than cash is 14.1% for debit cards, 13.4% for credit cards, 8.2% for electronic transfers of funds and 1.8% for checks. The main reason for the use of cash is the absence of point-of-sale terminals at commercial establishments. Considering that the retail-payment market worldwide is influenced by constant innovation in payment services, by the modernization of clearing and settlement systems, and by the efforts of regulators to redefine the payment industry for the future, these trends are addressed in the fourth section of the report. There is an account of how innovations in technology-based financial payment services have developed, and it shows that while this topic is not new, it has evolved, particularly in terms of origin and vocation. One of the boxes that accompanies the fourth section deals with certain payment aspects of open banking and international experience in that regard, which has given the customers of a financial entity sovereignty over their data, allowing them, under transparent and secure conditions, to authorize a third party, other than their financial entity, to request information on their accounts with financial entities, thus enabling the third party to offer various financial services or initiate payments. Innovation also has sparked interest among international organizations, central banks, and research groups concerning the creation of digital currencies. Accordingly, the last box deals with the recent international debate on issuance of central bank digital currencies. In terms of the methodological progress that has been made, it is important to underscore the work that has been done on the role of central counterparties (CCPs) in mitigating liquidity and counterparty risk. The fifth section of the report offers an explanation of a document in which the work of CCPs in financial markets is analyzed and corroborated through an exercise that was built around the Central Counterparty of Colombia (CRCC) in the Colombian market for non-delivery peso-dollar forward exchange transactions, using the methodology of network topology. The results provide empirical support for the different theoretical models developed to study the effect of CCPs on financial markets. Finally, the results of research using artificial intelligence with information from the large-value payment system are presented. Based on the payments made among financial institutions in the large-value payment system, a methodology is used to compare different payment networks, as well as to determine which ones can be considered abnormal. The methodology shows signs that indicate when a network moves away from its historical trend, so it can be studied and monitored. A methodology similar to the one applied to classify images is used to make this comparison, the idea being to extract the main characteristics of the networks and use them as a parameter for comparison. Juan José Echavarría Governor
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