Teses / dissertações sobre o tema "Benzylic derivatives"
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Bresciani, Stefano. "Stereospecific dehydroxyfluorination and the synthesis of trifluoro D-hexose sugar analogues". Thesis, University of St Andrews, 2011. http://hdl.handle.net/10023/1878.
Texto completo da fontePierret, Alexandre. "Fonctionnalisation à distance par métallotropie de dérivés benzyliques". Electronic Thesis or Diss., Université de Lorraine, 2023. https://docnum.univ-lorraine.fr/ulprive/DDOC_T_2023_0032_PIERRET.pdf.
Texto completo da fonteThis thesis presents a development of the remote functionalization reaction by metallotropic rearrangement on benzyl derivatives. The work is based on the use of a single metal reagent, a lithium triorganozincate, which allows the formation of two bonds C(sp3)-C(sp2) and C(sp3)-C(sp3) on sites 5 atoms apart in a single operation. The first chapter focuses on benzyl derivatives with an iodine in position 4 of the aromatic ring. Novel reaction conditions based on the use of a bio-based solvent are proposed. They allow to reach an unprecedented synthetic scope for such a reaction from these substrates. The influence of the solvent is also discussed. The second chapter is devoted to the mechanistic study by DFT of each step composing the reaction sequence studied previously. Thus, the halogen/metal exchange, the 1,2-migration of ligand or the metallotropic rearrangement are investigated with careful consideration of the solvent of the reaction. An experimental contribution completes this study. Finally, the extension of this transformation to benzylic heteroaromatic derivatives, in particular thiophenes, is the subject of the last chapter of this thesis. The reported work defines an approach of remote functionalization where a same toolbox, composed of a unique platform (halogenated thiophene bearing a benzyl phosphate) and an organometallic reagent of the same nature (lithium organozincate), offers several synthetic opportunities according to the experimenter's desires
Jaafar, Amani. "Synthèse, Caractérisation et Activité biologique des complexes à base de thiosemicarbazone". Thesis, Angers, 2017. http://www.theses.fr/2017ANGE0011/document.
Texto completo da fonteThiosemicarbazide and 4-methylthiosemicarbazide react with benzaldehyde derivatives by condensation to give different thiosemicarbazone ligands. The latter conduct in ethanolic medium to various complexes by reacting with chlorides and / or bromidesof copper (II), nickel (II), zinc (II), cobalt (II) and cadmium (II). The structures of the ligands and their complexes have been determined mainly by crystallography and by infrared spectroscopy, as well as by elementary analyzes. The ligands are in thion form in solid form.The complexes obtained are either monodentate, mononuclear or polynuclear complexes with two sulfur atoms of the thiosemicarbazone group, such as the determination of the crystal structure has shown either bidentate complexes with coordination sites, imine nitrogen and sulfur of the thio group. Their antifungal properties have been tested against human pathogenic strains: Aspergillus fumigatus, Candida albicans, C. glabrata, C. tropicalis, C. krusei, C. parapsilosis and Exophiala dermatitidis. Only thecomplexes with cadmium exhibited significant activities against the fungal species studied and the thiosemicarbazone of p-dimethylaminobenzaldehyde ligand almost completely inhibited the growth of E. dermatitidis
Lenihan, Brian David. "Generation of o-quinodimethanes from derivatives of trimethyl (o- ((p-tolylsulfonyl)methyl)benzyl)silane : a synthetic equivalent for the o-quinodimethant-[alpha], [alpha]- /". The Ohio State University, 1992. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487780393267272.
Texto completo da fonteAbou-Elkhair, Reham A. I. "Synthesis of anthraquinone derivatives and their conjugates with 2'-deoxynucleosides as new probes for electron transfer studies in DNA". unrestricted, 2008. http://etd.gsu.edu/theses/available/etd-07182008-154942/.
Texto completo da fonteTitle from file title page. Thomas L. Netzel, Dabney W. Dixon, committee co-chairs; David Boykin, Jerry Smith, committee members. Electronic text (250 p. : ill. (some col.)) : digital, PDF file. Description based on contents viewed Nov. 20, 2008. Includes bibliographical references.
Pham, Van Tuyet. "The synthesis and reactions of chiral 1,3,2-oxazaphospholane derivations : kinetic and mechanistic studies of polyether omega-phase catalyzed reactions of potassium cyanide with benzyl bromide in non-polar, aprotic solvent toluene". Diss., Georgia Institute of Technology, 1987. http://hdl.handle.net/1853/27416.
Texto completo da fonteMetzger, Albrecht [Verfasser]. "Preparation and applications of benzylic zinc chlorides : lewis-acid promoted additions of organomagnesium and organozinc reagents to carbonyl derivatives ; transition metal-catalyzed cross-coupling reactions with methylthio-substituted N-heterocycles / von Albrecht Metzger". 2010. http://d-nb.info/1003615341/34.
Texto completo da fonteChang, Ren-Chieh, e 張仁傑. "Design and Synthesis of Benzyl Caffeate Derivatives as JAK2 Inhibitors". Thesis, 2011. http://ndltd.ncl.edu.tw/handle/96461041056529506594.
Texto completo da fonte國立陽明大學
生物藥學研究所
99
JAK (Janus kinase) is a cytokine-induced kinase that activates STAT (Signal Transducer and Activator of Transcription) on many kinds of physiological effect such as cell proliferation, differentiation, and angiogenesis. Literature has been shown that over-activated JAK2/STAT3 pathway leads to highly transcription of oncogenes in various cancers, including solid tumor (e.g., liver, breast) as well as hematological malignancies. A series of JAK2 inhibitors have been developed and some of the inhibitors have been tested in clinical trial. Therefore, development of small molecule inhibitors for JAK2 is a promising strategy in cancer therapy. In this thesis, we applied the caffeate scaffold and X-ray structure of JAK2 to design and synthesize caffeate analogues. The inhibitory effect IC50 of these compounds was examined in HCC cell line. The MTT result shows that 6-bromopyridine in R2 position and hydrophobic ring (e.g., naphthalene) in R1 position enhances potency in cell cyto-toxicity. The structure-activity relationship provides the hints to develop new potent inhibitors.
Lo, mei ting, e 羅美婷. "Apoptosis induced by 1-benzyl carbazole-4-carboxaldehyde derivatives in human leukemia cell lines". Thesis, 2001. http://ndltd.ncl.edu.tw/handle/90007866802222515218.
Texto completo da fonte中國醫藥學院
藥物化學研究所
89
Abstract Synthesized 1-benzyl carbazole-4-carboxaldehyde derivatives ( LCY ) examined for their growth inhibition effects in human leukemia cell lines. HL60, U937, and K562 cells were treated with these compounds for 24 hours and their proliferation was determined by the propidium iodide DNA staining method. A dose-dependent decrease in the cell proliferation rate was observed for all compounds. LCY-12 had the highest growth inhibitory, and its IC50 were 2.58, 0.77, and 19.49 μM for HL60, U937, and K562 cells, respectively. DAPI-stained cells revealed evident characteristics of apoptosis, which include cell shrinking, chromatin condensation, fragmentation of nuclei, and formation of apoptotic bodies. DNA from treated HL60 and U937 cells displayed a characteristic inter-nucleosomal ladder of DNA fragments. Furthermore, down-regulation of Bcl-2, up-regulation of Bax, activation of caspase 3, 8, and 9, and cleavage of PARP were detected by Western blotting method in LCY-12-treated HL60 cells. Caspase inhibitors significantly reduced LCY-12-induced caspase activity and cell death. In addition, LCY-12 and LCY-16 induced G2/M arrest in HL60 cells, and S arrest in U937 cells. The induction of cell cycle arrest occurred before the onset of apoptosis. Western blotting analysis of cyclins and CKIs revealed that LCY-12 induced the expression of cyclin B, cdc25c and p21 proteins. These results indicated that the ability of LCY-12 to inhibit cell proliferation may be mediated by the induction of apoptosis and cell cycle arrest.
Huang, Chun-Lung, e 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.
Texto completo da fonte中國醫藥大學
藥物化學研究所碩士班
94
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 Schotten-Baumann reaction to give 22a-h, 23a-h, 24 and 25, respectively. The last, intermediate 22a-h, 23a-h, 24, 25 are cyclizated by amberlyst A-26 resin (OH- form) and then acidified with trifluroacetic acid to obtain 26a-g, 27a-g, 28 and 29, respectively. Moreover, it is important to evaluate the biological activity from the derivatives, anticipating obtaining leading compounds to establish the structure-activity relationships.
Yang, Ju-Ying, e 楊如盈. "Transformation of D-(-)-quinic acid into 3,4,6-trihydroxyazepanes and their N-benzyl derivatives for potential glycosidase inhibitors". Thesis, 2005. http://ndltd.ncl.edu.tw/handle/00627216705643635736.
Texto completo da fonte淡江大學
化學學系碩士班
93
The naturally occurring five- and six-membered azasugars are considered as glycosidase inhibitors. Most recently, the seven-membered azasugars(poly-hydroxyazepanes) were reported to have potential in treatment of diabetes, cancers and AIDS. These heterocycles are more flexible in conformation than the corresponding six- and five-membered counterparts and may bind in the minor groove of DNA. Little attention has been given to trihydroxyazepanes. We wish to describe herein a new approach to the synthesis of diastereomeric azasugars (3,4,6-trihydroxyazepanes) in ten steps each from the commercially available D-(-)-quinic acid. The biological test of this series of 3,4,6-trihydroxyazepanes and their derivatives allows us to compare with their corresponding tetrahydroazepanes. Especially, we can further learn the structure relationship regarding to the stereochemistry of hydroxy groups.
Tsai, Shang-Cheng, e 蔡尚宬. "I. Synthesis of D-amino acid derivatives from camphorII . Preparation of 1-benzyl indenones from 1-indanone". Thesis, 2019. http://ndltd.ncl.edu.tw/handle/79a39r.
Texto completo da fonte國立暨南國際大學
應用化學系
107
I、Most of the natural amino acids are mainly L-amino acids, and the D-amino acids are the enantiomers of L-amino acids, which can be incorporated into the peptides to adjust their biological activities. In this laboratory, we used the camphor as the starting material for the Witting reaction, the oxidation reaction, the ring expansion reaction and the reduction reaction to obtain the organic catalyst based on camphor. On this basis, we used palladium metal as the catalyst after the hydrogenation expansion product. The hydrogenated product is obtained, and then pyridine is added as a solvent acetic anhydride, followed by reaction with Iodosobenzene diacetate and Potassium hydroxide to obtain a corresponding product, and then ring-opening reaction is carried out to successfuliy cyclopentanyl D-Amino Acid 57. II、Many structures in nature have a bicyclic structure. Due to the rare amount of such natural substances and antibacterial effects, such as: Pallidol, these two specific monomers have been found to have antibacterial functions, so we have used the laboratory to publish The basic basis for a series of compounds in one pot, it is desirable to shorten the steps and obtain novel phenylcarbonyl olefins without the use of a metal catalyst.
Chen, Hua-Sin, e 陳華鑫. "Synthesis and biological activities of ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3) derivative". Thesis, 2008. http://ndltd.ncl.edu.tw/handle/47453222969722384672.
Texto completo da fonte中國醫藥大學
藥物化學研究所
96
In the previous study, ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3) was identified as the first selective non-peptide protease-activated receptor 4 (PAR4) antagonist. In order to develop noel PAR4 antagonist, YD-3 was selected as lead compound. Two series of N1-substituted arylmethyl-3-(4-ethoxycarbonylphenyl)indazole derivatives (I) and N2-substituted arylmethyl-3-(4-ethoxycarbonylphenyl)indazole derivatives (II) were synthesized. The key intermediate, ethyl 4-(1H-indazol-3-yl)- benzoate (8) was prepared according to the know method. Then, compound 8 was subjected to alkylation with directly substitution or Mitsunobu reaction to yield corresponding N1-substituted arylmethyl derivatives (I) as major products. However, the microwave-assisted synthetic technique can be successfuly promote N2- substituted arylmethyl derivatives (II) as major products. The synthesized compounds were evaluated for their selective anti-protease- activated receptor 4 (anti-PAR4) activity. Through structure-activity relationships (SAR) study the functional groups contributing to anti-PAR4 activity was identified. Several new compounds with anti-PAR4 activity comparable to YD-3 were found. Among them, ethyl 4-[1-(3-chlorobenzyl)-1H-indazol-3-yl]benzoate (71) showed the most potent inhibitory effect on PAR4-mediated platelet aggregation. Compound 71 is worthy of further investigation. In addition, the synthesized compounds were examined for their anti- inflammatory, anti-allergic, cytotoxic, and anti-bacterial activity. Among these tested compounds, methyl 4-(1H-indazol-3-yl)benzoate (6) and 4-(1-benzyl-1H-indazol-3- yl)-N-hydroxybenzamide (23) showed the better inhibitory effect of LPS induced TNF-α formation than positive control SB-203580 (IC50≒4.8?b2.4 and 2.1?b0.2 μM, respectively). Compounds 8, 4-[1-(2-fluorobenzyl)-1H-indazol-3-yl]-N-hydroxy benzamide (117), 4-[1-(3-fluorobenzyl)-1H-indazol-3-yl]-N-hydroxybenzamide (118), 4-[1-(2-methoxybenzyl)-1H-indazol-3-yl]-N-hydroxybenzamide (120), 4-[1-(3- methoxybenzyl)-1H-indazol-3-yl]-N-hydroxybenzamide (121), and 4-[1-(4-methoxy benzyl)-1H-indazol-3-yl]-N-hydroxybenzamide (122) showed the better inhibitory effect of LPS induced TNF-α formation than positive control genistein (IC50≒1.7?b0.8, 2.4?b0.7, 1.7?b0.2, 3.5?b0.5, 3.5?b0.4, and 2.9?b1.3 μM, respectively). 4-[1-(3-Chlorobenzyl)-1H-indazol-3-yl]-N-hydroxybenzamide (115) showed the better inhibitory effect of fMLP/cytochalasin B induced neutrophil superoxide formation than positive control DPI (IC50≒1.2?b1.1, 0.8±0.2, 1.3±0.6, and 2.0±0.6 μM, respectively). 4-(1-Benzyl-1H-indazol-3-yl)benzamide (17) and 4-(1-benzyl-1H- indazol-3-yl)-N-hydroxybenzamide (23) showed the better inhibitory effect for β-glucuronidase expression of fMLP/cytochalasin B induced neutrophil degranulation than positive control genistein (IC50≒6.4?b1.1 and 1.6?b0.5 μM, respectively). Methyl 4-(4,5,6,7-tetrahydro-1H-indazol-3-yl)benzoate (5), 6, ethyl 4-(2-benzyl-2H-indazol- 3-yl)benzoate (11), 4-(1-benzyl-1H-indazol-3-yl)benzoic acid (12), 17, 23, 135, and methyl 4-(2-benzyl-2H-indazol-3-yl)benzoate (137) showed the better inhibitory effect for lysozyme expression of fMLP/cytochalasin B induced neutrophil degranulation than positive control genistein (IC50≒8.6?b0.6, 8.9?b0.6, 8.7?b1.4, 15.0?b0.6, 4.7?b1.2, 4.0?b0.4, 12.0?b1.3, 11.7?b1.2, 10.5?b2.1, and 9.1?b1.1 μM, respectively). Compounds 8, 117, and [4-(1-benzyl-6-methoxy-1H-indazol-3- yl)phenyl]methanol (134) showed the better inhibitory effect for β-glucuronidase expression of fMLP/cytochalasin B induced neutrophil degranulation than positive control TFP (IC50≒8.4?b2.6, 5.7?b1.4, and 9.4?b0.8 μM, respectively). Compounds 8, showed the better inhibitory effect for lysozyme expression of fMLP/cytochalasin B induced neutrophil degranulation than positive control TFP (IC50≒3.9?b2.3 μM). They were found to exhibit significant anti-inflammatory activity and were selected as new lead compounds. Besides, compounds 92, 4-[1-(3-chlorobenzyl)-1H-indazol- 3-yl]benzoic acid (93), 4-[1-(3-fluorobenzyl)-1H-indazol-3-yl]benzoic acid (96), 115, and 118 were found to exhibit significant anti-bacterial activity against Staphylococcus aureus ATCC 25923, Staphylococcus aureus 1, and Staphylococcus aureus 2.
Tsai, Ray-Ying, e 蔡睿盈. "Synthesis,Antiplatelet,Antiangiogenesis and Cytotoxicity Activity of 1-Benzyl-3-(5-substituted-2-furyl)-5-methoxy-1H-indazole Derivatives". Thesis, 2003. http://ndltd.ncl.edu.tw/handle/68278761980375752184.
Texto completo da fonte中國醫藥學院
藥物化學研究所
91
Abstract 1-Benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (YC-1) was first synthesized in our laboratory as a novel antiplatelet agent. Encouraged by the initial results, a series of 5-methoxy derivatives of YC-1 analogues were synthesized and examined for their biological activities. The starting material methyl 5-(3-methoxybenzoyl)-2-furoate (1) was treated with benzylhydrazine to yield a mixture of E- and Z-form isomers 2. The hydrazone was then treated with lead tetraacetate in dichloromethane at low temperature, then boron trifluoride etherate was added and the mixture heated to form the expected key intermediate :methyl 5-(1-benzyl-5-methoxy-1H-indazol-3-yl)-2-furoate (4). Starting from methyl 5-(1-benzyl-5-methoxy-1H-indazol-3-yl) -2-furoate (4), various esters 8a—8d、amides 9a—9h and amino acid methyl esters 10a—10f were synthesized,biological evaluation of the synthesized compounds are currently under investigation.
Yu, Michael Seungju. "Smectic ordering of rod-like polymers owing to monodispersity of chain length: Synthesis and characterization of benzyl and (4-hexadecyloxy)benzyl esters of monodisperse derivatives of poly(alpha,L-glutamate)". 1998. https://scholarworks.umass.edu/dissertations/AAI9909234.
Texto completo da fonteChou, Hua-Cheng, e 周華晟. "Designed to Synthetic Benzyl Ether-Linked Glucuronide Derivative of Benzo[de]quinoline camptothecin(BQC) for Selective Anticancer Therapy". Thesis, 2013. http://ndltd.ncl.edu.tw/handle/17913684817324924372.
Texto completo da fonte嘉南藥理科技大學
藥學系
101
5, 6-Dihydro-4H-benzo[de]quinolone camptothecin (BQC), a derivative of camptothecin, has been identified as a potential anti-tumor drug. Additionally, BQC could be conjugated with a methyl glucuronate to improve its tumor specificity and also its water solubility. Dr. Masamichi. firstly synthesized compound 6 from compound 1 through nitrification, oxidation and reduction. Compound 6 then was conjugated with compound 7 to give BQC. However, when the start material is compound 1, the nitrification step would produce a 6-nitro and 6, 8-dinitro byproduct, thus it requires purification of the 8-nitro main product. The yield of nitrification and oxidation is 13.0% and 77.4%, respectively, the total yield is just 10%. In our study, in order to increase the total yield, we modified the synthesis process. We obtained compound 5 by using the same starting material (compound 1) but with different orders, which are oxidation and nitrification. The yield of oxidation and nitrification is 42.7% and 69%, respectively. The total yield is 33%. It is 3-folds better than the original process. In order to improve the practicality of clinical applications by increased the tumor targeting, we were according to the strategy of prodrug. We have been designed and synthesized a BQCG -ester type compound.
Soto, Carissa M. "Monodisperse benzyl -ester derivatives of poly(α, L-glutamate) and poly(α, L-aspartate) modeling nature's delicate state of matter". 2000. https://scholarworks.umass.edu/dissertations/AAI9960791.
Texto completo da fonte