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Dissertations / Theses on the topic '1;2;4-triazole derivatives'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

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

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2

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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3

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, hig

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4

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

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5

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, l

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6

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

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7

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

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8

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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9

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

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10

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 towa

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11

Huang, Chun-Lung, and 黃俊龍. "Synthesis and biological activity of 1-benzyl-4-hydroxy-3-phenylquinolin-2(1H)-one derivatives." Thesis, 2006. http://ndltd.ncl.edu.tw/handle/37426286995940238871.

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碩士<br>中國醫藥大學<br>藥物化學研究所碩士班<br>94<br>The dissertation is based on the structure of 4-hydroxy- quinolin-2-(1H)-ones. In order to synthesize a series of derivatives of 1-benzyl-4-hydroxy-3-phenylquinolin-2(1H)-one (26a-g, 27a-g, 28, 29), Using the Bheemashankar′s solution-phase combinatorial synthetic method. The starting material is methyl anthranilate (16) that is condensated with 4-substituted-benzaldehydes 17a-h to obtain the 19a-h. On the other hand, 4-cyanophenyl acetic acids 20a-d were acylated with thionyl chloride to afford acid chlorides 21a-d. Then, 21a-d and 19a-h are combined by Scho

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12

Rico, Duque Jenny Lorena. "Synthesis of 1,2-methano-tetrahydrofuran derivatives and 1´,2´-methano-2´,3´-dideoxynucleosides as potential antivirals." Thèse, 2018. http://hdl.handle.net/1866/20042.

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13

CHEN, WEN-TONG, and 陳文童. "The study of conducting polymer solid-state polymerization of 2, 4-hexadiyne-1, 6-diol and its derivatives." Thesis, 1989. http://ndltd.ncl.edu.tw/handle/06051250112823735202.

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14

Chang, YuanBao, and 張元寶. "Synthetic Studies on 4-Amino-1-[(hydroxyureido)alkyl]-2-quinazolinones and Their Derivatives as Potential HCV NS3 Helicase Inhibitors." Thesis, 2000. http://ndltd.ncl.edu.tw/handle/60261666896350415020.

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碩士<br>國立臺灣大學<br>藥學研究所<br>88<br>Hepatitis C virus (HCV), a virus that infects some 170 million people worldwide, is causing rising rates of liver disease. The necessity of finding potent anti-HCV agents is an urgent task. Hydroxyurea was reported to possess antiviral and antitumor activities as the results of inhibiting DNA synthesis. It is also an analogue of hydroxamic acid, a well-known compound with high affinity for metal ions. These make it of value in the development of anti-HCV agents. In this investigation, a novel series of quinazolinone derivatives comprise of hydroxyurea moiety, suc

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15

Fang, Yu-Wen, and 方昱文. "Synthesis and Biological Evaluation of (2-(4-Phenyl)-1,3-butadien-1-yl)quinoline-8-ol Derivatives as Anticancer Agents." Thesis, 2013. http://ndltd.ncl.edu.tw/handle/71505737422723661754.

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碩士<br>高雄醫學大學<br>醫藥暨應用化學研究所<br>101<br>(E)-2-(2-(5-nitrofuran-2-yl)vinyl)quinolin-8-ol (HZY-2023) has demonstrated a strong inhibitory effect on difficult ablation period of prostate cancer cells. However, its cytotoxity against normal cells prevents further application. In this study, the alkene between two aromatic rings was replaced by diene to alter the redox properties. This modification improve inhibitory effect and reduced the normal toxiaty aginst cell. The results of biological assay indicated series of derivatives which exhibit selectively cytotoxity against androgen-independent and re

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16

Chen, Yu-Jen, and 陳俞臻. "(1) Temperature and Matrix Effects Dependence on the Triplet Radical Pairs Generated from Photolysis of N-Tosylpyrrole Derivatives, (2) Photochemistry of Heteroaromatic Fused ??-1,2,3-Triazoline Derivatives, (3) Application of Tetrazole Modified Calix[4]a." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/54411936287525538177.

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博士<br>國立交通大學<br>應用化學研究所<br>98<br>In part 1, the photolysis (230-325 nm) of N-tosyl pyrrole 37, 2-phenyl-N-tosyl pyrrole 72, 2,5-diphenyl-N-tosyl pyrrole 73, and N-(2-naphthyl)-sulfonyl pyrrole 75 in a 2-methyltetrahydrofuran glassy matrix at 4 K gives electron paramagnetic resonance (EPR) spectra with triplet characteristics; the zero-field-splitting (zfs) parameters D' for the corresponding radical pairs (RPs) 93, 94, 95, and 96 are 0.0239, 0.0190, 0.0174, and 0.0241 cm-1, respectively. Irradiation of 37 at RT allows the isolation of two rearranged products 38 and 39 and a polymeric material

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17

Lin, Chia-Hui, and 林佳慧. "Synthesis and Optimization of 2-(1-Ethyl-3,5-dimethyl-1H-pyrazol-4-yl)ethan-1-amine Derivatives with in Vitro Activity against Triple-Negative Breast Cancer Cells." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/77382163953235178318.

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碩士<br>國立中央大學<br>化學學系<br>104<br>Triple negative breast cancer (TNBC) has high mortality rate, high recurrence and high brain metastasis. Chemotherapy is the only treatment, and the worst of all it develops drug resistance. Therefore, we devote to drug discovery and synthesis for alleviating the suffering of patients. According to the previous research, the derivatives of pyrazole scaffold have activity against cancer. Hence, we study pyrazole compound N-(2-(1-ethyl-3,5-dimethyl-1H-pyrazol-4-yl)ethyl)-4-isobutyl- N-methylbenzenesulfonamide (YL-18), which is chosen as the hit compound through hig

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18

Smith, Emilie Despagnet. "Part I. Study of 1-acyl-2-dimethylphenylsilyl-2,3-dihydro-4-pyridone as synthetic intermediates ; Part II. Synthesis of enantiopure nicotine derivatives from nicotine." 2004. http://www.lib.ncsu.edu/theses/available/etd-07012004-172421/unrestricted/etd.pdf.

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19

Tsau, Yu-Shuo, та 曹育碩. "一、Lewis Acid-Promoted Intramolecular Cyclization of Silyl-Protected 3-(3-Arylpropargyltosylamino)methylcyclohex-2-en-1-ols: Synthesis of Azaspiro[4.5]dec-6-ene Derivatives 二、Brønsted Acid-Catalyzed and Lewis Acid-Assisted Intramolecular Cyclization of 2-Methyl-2,3-epoxy-4-(3-arylpropargyl)cyclohexan-1- ones: Synthesis of 7-Benzoylbicyclo[3.2.1]octan-2-one and Ar-yl(halo)methylenebicyclo[3.2.1]octan-2-one Derivatives". Thesis, 2014. http://ndltd.ncl.edu.tw/handle/59021650894423613213.

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碩士<br>國立臺灣師範大學<br>化學系<br>102<br>This thesis focuses on acid-promoted intramolecular cyclization of O-silyl-protected 3-(3-arylpropargyltosylamino)methylcyclohex-2-en-1-ols and 2-methyl-2,3-epoxy-4-(3-arylpropargyl)cyclohexan-1-ones. Two major reactions are discussed. First, BF3•OEt2-promoted intramolecular cyclization/ fluorination of O-silyl-protected 3-(3-arylpropargyltosylamino)methylcyclo- hex-2-en-1-ols at room temperature under an atmosphere of nitrogen afforded N-containig spiro[4.5]dec-6-ene derivatives containing a C(sp2)-F bond. In this process, boron trifluoride diethyl etherate act

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20

Prince, Ashleigh Lauren. "Homogeneous and Heterogeneous Approaches to 1,2,4-Triazine-Accelerated Copper-Catalyzed Azide-Alkyne Cycloadditions." 2011. http://trace.tennessee.edu/utk_graddiss/1117.

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Over the last decade, the domain of click chemistry has grown exponentially and has significantly impacted the fields of organic synthesis, medicinal chemistry, molecular biology, and materials science. The ideal model of a click reaction has become the copper-catalyzed azide-alkyne cycloaddition (CuAAC). Inherent limitations of CuAAC, including high temperatures, long reaction times, and difficult purifications, have been minimized by the development of nitrogen-based ligands. Herein, we present a novel application of 1,2,4-triazines by investigating their use as accelerants for CuAAC. A d

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21

Chaudhary, Arpana S. "Inhibitors of SecA as Potential Antimicrobial Agents." 2013. http://scholarworks.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

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22

Yang, Fu-Ming, and 楊富名. "(1) Syntheses and Optical Resolution of Inherently Chiral Fluorescent Calix[4]arenes and Their Chiral Recognition (2) Syntheses of Calix[4]arenes with Lower-rim Anthryl-triazole and Ester Groups for Metal Ions Sensing Studies." Thesis, 2010. http://ndltd.ncl.edu.tw/handle/33838972847607299254.

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碩士<br>國立交通大學<br>應用化學研究所<br>98<br>In this thesis, my research is focused on two topics. the first part is the synthesis and optical recognition of fluorescent inherently chiral calix[4]arenes and their chiral recognition. The second part is the synthesis of cailx[4]arenes with lower-rim triazole and ester groups as cationic binding site and anthracene as the fluorophores. 　　In part one, we synthesized novel calix[4]arene of AABH-type with inherent chirality through the reaction of racemic calix[4]arene derivatives 40a and 40b with 1-phenylethylamine (both R-form and S-form), follow by the separ

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