Relevant bibliographies by topics / Bioactive compounds - Synthesis

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  1. Journal articles
  2. Dissertations / Theses
  3. Books
  4. Book chapters
  5. Conference papers

Academic literature on the topic 'Bioactive compounds - Synthesis'

Author: Grafiati
Published: 4 June 2021
Last updated: 25 January 2023

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Journal articles on the topic "Bioactive compounds - Synthesis"

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Suryaningtyas, Indyaswan Tegar. "SENYAWA BIOAKTIF MIKROALGA DAN PROSPEKNYA DI MASA DEPAN." OSEANA 44, no. 1 (April 30, 2019): 15–25. http://dx.doi.org/10.14203/oseana.2019.vol.44no.1.28.

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BIOACTIVE COMPOUND FROM MICROALGAE AND ITS FUTURE PROSPECT. Microalgae biomass is potential to be used in various fields, one of which is as a producer of bioactive compounds. Bioactive compounds from microalgae can be used extensively in the pharmaceutical industry, cosmetic’s raw materials, food flavouring substances, and functional food ingredients. In terms of health, the bioactive compounds have the potential as antioxidants, antiviral, antibacterial, anti-fungal, anti-inflammatory, anti-tumor, and prevent the effects of malaria, but the potential for microalgae’s bioactive compound has not been explored well if compared to the production of terrestrial plants. Some examples of the bioactive compounds that have been used are carotenoid groups such as lutein, β-carotene, astaxanthin and fucoxanthin; fatty acid groups such as EPA and DHA; and also some toxin compounds such as domoic acid. To obtain the optimum yield of bioactive compounds, it requires the right method in biomass production, compound extraction, compounds isolation and compounds identification. While testing the activities, it is necessary to do some assays such as antioxidan, antibiotic, antiviral and anticancer assay. The development of the technology can improve the potential use of microalgae to synthesis its bioactive compounds.
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Trabocchi, Andrea. "Design and synthesis of bioactive compounds." Bioorganic & Medicinal Chemistry 25, no. 19 (October 2017): 5031. http://dx.doi.org/10.1016/j.bmc.2017.09.020.

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Susanto, Edy, Anik Fadlilah, and Muhammad Fathul Amin. "Synthesis, extraction and idetification of meat bioactive peptides: a review." IOP Conference Series: Earth and Environmental Science 888, no. 1 (November 1, 2021): 012058. http://dx.doi.org/10.1088/1755-1315/888/1/012058.

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Abstract The consumption of meat should consider the concept of functional food. The meat had a highquality protein and contain of bioactive peptide compounds. Amino acid was component of bioactive peptides compound. It joined by covalent bonds known as amide or peptide bonds. A lot of research was currently focused on the bioactive peptide compounds isolated from myofibril and sarcoplasmic proteins with the synthesis, extraction, and identification methods. This study used a systematic review to get the structure of amino acids that the source of bioactive components and the principle of synthesis, extraction and identification of bioactive peptide in the meat. This paper highlights were finding on the structure of amino acid in the meat. The proportion of amino acids was also different in each animal body location. The result identified that more than 170 peptides were released from the main structure of the myofibril (actin, myosin) and sarcoplasmic muscle proteins, and the synthesis, extraction and bioactive peptide identification in the meat as well as their potential use as functional food.
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Tatsuta, Kuniaki. "Significance of Total Synthesis of Bioactive Compounds." Current Organic Chemistry 5, no. 2 (February 1, 2001): 207–31. http://dx.doi.org/10.2174/1385272013375670.

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ISOBE, Minoru. "Stereocontrolled Synthesis of Multi-Functional Bioactive Compounds." Journal of Synthetic Organic Chemistry, Japan 55, no. 1 (1997): 44–55. http://dx.doi.org/10.5059/yukigoseikyokaishi.55.44.

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Resnati, Giuseppe. "Synthesis of chiral and bioactive fluoroorganic compounds." Tetrahedron 49, no. 42 (1993): 9385–445. http://dx.doi.org/10.1016/s0040-4020(01)80212-x.

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Garcı́a-Junceda, Eduardo, Juan Francisco Garcı́a-Garcı́a, Agatha Bastida, and Alfonso Fernández-Mayoralas. "Enzymes in the synthesis of bioactive compounds." Bioorganic & Medicinal Chemistry 12, no. 8 (April 2004): 1817–34. http://dx.doi.org/10.1016/j.bmc.2004.01.032.

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Melford C Egbujor, Uchechukwu C Okoro, Samuel A Egu, Pius I Egwuatu, Florence U Eze, and Ifeanyi S Amasiatu. "Synthesis and Biological Evaluation of Alanine Derived Bioactive p-Toluenesulphonamide Analogs." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (October 19, 2020): 6449–58. http://dx.doi.org/10.26452/ijrps.v11i4.3440.

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Sulphonamides and carboxamides have great pharmacological importance. The purpose of the study was to synthesize alanine-derived bioactive sulphonamides bearing carboxamides and evaluate their biological activities. The reaction of p-toluenesulphonyl chloride with L-alanine afforded compound 1, which was acetylated to obtain compound 2. The chlorination and ammonolysis of compound 2 gave the carboxamide backbone (3) which was coupled with aryl/heteroaryl halides to afford the hybrid compounds 4, 5 and 6. Structures were confirmed by FTIR, 1H-NMR, 13C-NMR spectra and elemental analytical data. The in vitro antimicrobial properties were determined by agar dilution, and the antioxidant properties were also investigated. Molecular docking interactions of the analogues were determined using PyRx. Compounds 4, 5 and 6 exhibited excellent in vitro antimicrobial properties in the range of 0.5-1.0mg/ml while compounds 1and 2 had half-maximal inhibitory concentration (IC50) of 1.11±0.15µg/ml and 1.12±0.13µg/ml respectively. For the molecular docking studies, compounds 5 and 6 displayed the best antitrypanosomal activity with binding affinities of -13.95 and -13.51kcal/mol respectively while compound 4 showed the highest in silico antimalarial activity having binding affinity of -11.95kcal/mol. All the alanine derived sulphonamides were observed to be potential antimicrobial, antioxidant, antitrypanosomal and antimalarial agents following the biological activities studies.
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Lee, Hing-Ken, Kin-Fai Chan, Chi-Wai Hui, Ho-Kee Yim, Xun-Wei Wu, and Henry N. C. Wong. "Use of furans in synthesis of bioactive compounds." Pure and Applied Chemistry 77, no. 1 (January 1, 2005): 139–43. http://dx.doi.org/10.1351/pac200577010139.

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Synthetic approaches to the total synthesis of plakortone B, as well as diastereoselective nucleophilic additions to furyl aldehyde and furyl sulfonylimine employing chiral 3-boronates as auxiliary are presented.
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Khan, Ayad Kareem, Suaad Mohammed Hussain, Mohammed Rifat Ahmad, Fitua Manwar Aziz, and Shimaa Mutasim Abdulah***. "Synthesis, Characterization and Antimicrobial Screening of Some Bioactive 1,8-Naphthalimide Derivatives." Al Mustansiriyah Journal of Pharmaceutical Sciences 14, no. 2 (December 1, 2014): 33–47. http://dx.doi.org/10.32947/ajps.v14i2.145.

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This research include developing new heterocyclic derivatives of 1,8-naphthalimides bearing oxazoline, thiazoline, oxadiazole, thiadiazole and aminotriazole moieties as the following steps: N-ester-1,8-naphthalimide (1) was obtained by direct imidation of 1,8- naphthalic anhydride with ethylglycinate in dimethylsulfoxide. Compound (1) was treated with hydrazine hydrate in absolute ethanol to give N-acetohydrazide-1,8-naphthalimide (2).N-Acetophenylsemicarbazide-1,8-naphthalimide (3) and N-Aceto phenylthiosemicarbazide- 1,8-naphthalimide (7) were synthesized via reaction of compound (2) with phenylisocyanate and phenylisothiocyanate in absolute ethanol respectively.Cyclization of compounds (3) and (7) with p-substituted phenacyl bromide gives the oxazoline derivatives (4-6) and thiazoline derivatives (9-11) respectively. N-Methyl-[(5- (phenyl amino)-1,3,4-thiadiazol-2-yl)]-1,8-naphthalimide (8) prepared via treatment of compound (7) with phosphoric acid. Reaction of the prepared hydrazide (2) with carbon disulfide in the presence of potassium hydroxide producing N-Methyl-[potassium dithiocarbazate]-1,8-naphthalimide (12). Acidifying of the obtained salt (12) with 4N hydrochloric acid give N-Methyl-[1,3,4-oxadiazol-2-yl-5-thiol]-1,8-naphthalimide (13). The obtained salt (12) also treated with hydrazine hydrate to afford the desirable N-Methyl-[1,2,4- triazol-3-yl-4-amino-5-thiol]-1,8-naphthalimide (14).All the prepared compounds in this research were characterized by recording their melting points, FTIR, 1HNMR, 13CNMR spectra, checked by TLC, physical properties and some specific chemical tests also. Some of the new prepared compounds were evaluated for the antimicrobial screening in vitro against two types of Gram positive bacteria including (Staphylococcus aureus, Bacillus subtilis) and two types of Gram negative bacteria including (Escherichia coli, Pseudomonas aeuroginosa).More, antifungal activities of some prepared compounds performed against the yeastlike pathogenic fungus (Candida albicans). The antimicrobial screening carried out in three concentrations of prepared compounds. Sulfamethoxazole/Clotrimazole was used as standard drugs. The results showed that most of the tested compounds have good biological activity against the mentioned organisms compared with standard drugs above
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Dissertations / Theses on the topic "Bioactive compounds - Synthesis"

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Soldati, Roberto <1986&gt. "Synthesis of new bioactive β-lactam compounds." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2015. http://amsdottorato.unibo.it/6974/.

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New biologically active β-lactams were designed and synthesized, developing novel antibiotics and enzymatic inhibitors directed toward specific targets. Within a work directed to the synthesis of mimetics for RGD (Arg-Gly-Asp) sequence able to interact with αvβ3 and α5β1-type integrins, new activators were developed and their Structure-Activity Relationships (SAR) analysis deepened, enhancing their activity range towards the α4β1 isoform. Moreover, to synthesize novel compounds active both against bacterial infections and pulmonary conditions of cystic fibrosis patients, new β-lactam candidates were studied. Among the abundant library of β-lactams prepared, mainly with antioxidant and antibacterial double activities, it was identified a single lead to be pharmacologically tested in vivo. Its synthesis was optimized up to the gram-scale, and pretreatment method and HPLC-MS/MS analytical protocol for sub-nanomolar quantifications were developed. Furthermore, replacement of acetoxy group in 4-acetoxy-azetidinone derivatives was studied with different nucleophiles and in aqueous media. A phosphate group was introduced and the reactivity exploited using different hydroxyapatites, obtaining biomaterials with multiple biological activities. Following the same kind of reactivity, a small series of molecules with a β-lactam and retinoic hybrid structure was synthesized as epigenetic regulators. Interacting with HDACs, two compounds were respectively identified as an inhibitor of cell proliferation and a differentiating agent on steam cells. Additionally, in collaboration with Professor L. De Cola at ISIS, University of Strasbourg, some new photochemically active β-lactam Pt (II) complexes were designed and synthesized to be used as bioprobes or theranostics. Finally, it was set up and optimized the preparation of new chiral proline-derived α-aminonitriles through an enantioselective Strecker reaction, and it was developed a chemo-enzymatic oxidative method for converting alcohols to aldehydes or acid in a selective manner, and amines to relative aldehydes, amides or imines. Moreover, enzymes and other green chemistry methodologies were used to prepare Active Pharmaceutical Ingredients (APIs).
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Eaton, Alexander Lee. "Isolation and Synthesis of Bioactive Compounds from Plants." Diss., Virginia Tech, 2015. http://hdl.handle.net/10919/64367.

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As a part of a continuing search for bioactive compounds with the International Cooperative Biodiversity Group (ICBG), and in collaboration with the Natural Products Discovery Institute of the Institute for Hepatitis and Virus Research (IHVR), twelve plant extracts were investigated for their antiproliferative activity against the A2780 cell line, three plant extracts were investigated for their antimalarial activity against Plasmodium falciparum, and three plant extracts were investigated for their anti-inflammatory activity (PPAR-y inhibition). Bioassay-guided fractionation of extracts led to the identification of four new antiproliferative compounds (2.1-2.3, 3.1), five new anti-inflammatory compounds (6.4a, 6.5a-b, 6.6a, 6.6c), and twenty-eight known compounds from eight of the extracts. In addition, mallotojaponin C, an antimalarial natural product, and derivatives were synthesized and investigated for their antimalarial activity.
Ph. D.
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Chyan, Ming-Kuan. "Synthesis and Study of Bioactive Compounds: I. Pyrethroids; II. Glutathione Derivatives." Thesis, University of North Texas, 1995. https://digital.library.unt.edu/ark:/67531/metadc278848/.

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Part I: In the first study of pyrethroids, twenty-one novel pyrethroid esters bearing strong electron-withdrawing groups (e.g., halomethylketo and nitro groups) in the double bond side chain of the cyclopropane acid moiety have been synthesized and evaluated for insect toxicity. Rather than the usually employed Wittig reaction for these syntheses, the novel pyrethroid acid moieties were prepared by amino acidcatalyzed Knoevenagel condensations under mild conditions. In the second study of pyrethroids, fourteen pyrethroid-like carbonates were synthesized by condensation of a variety of alcohols and the chloroformates of the corresponding known pyrethroid alcohols.
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Trippier, Paul Charles. "Synthesis of highly substituted heterocycles : the oxazolomycins." Thesis, University of Oxford, 2006. http://ora.ox.ac.uk/objects/uuid:b758987c-7a0c-4c1b-982c-61b4d383680a.

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This thesis is concerned with studies towards the total synthesis of a class of natural products - the oxazolomycins. Attention was focused on the left-hand side triene fragment and right-hand side lactam heterocyclic system. This thesis describes the synthesis of a racemic terminal phenyl analogue of oxazolomycin A and C, possessing the left-hand side triene geometry as required. A novel truncated pyridine analogue is also described. The molecules represent a racemic total synthesis of analogues of phthoxazolin A and inthomycins B and C. The synthesis is based upon a crucial Stille cross-coupling reaction between stannane and diene iodide fragments. The stannane fragment was synthesised using literature precedented methods and the vinyl halide prepared using a highly stereoselective Wittig, Takai homologation or Stork reaction leading to a variety of ratios of mixtures of Z, E and E, E diene halides. These investigations led to the availability of 1:1, 3:1 and 1:3 mixtures of Z, Z, E : Z, E, E left hand side triene fragments possessing the required stereochemistries for oxazolomycin A and C. Utilising existing methodology developed in the Moloney group, investigations were carried out towards construction of β-keto esters possessing terminal hydroxyl functions, suitable for diastereoselective aldol ring closure. Following extensive protecting group manipulation and N-acylation coupling optimisation, a TIPS protected β-keto acid, existing as predominantly the keto tautomer, was successfully coupled to an oxazolidine heterocycle. This N-acylated oxazolidine upon Dieckmann cyclisation would present an advanced intermediate of opposite configuration (Lserine is used here as a cheaper starting material for the construction of the oxazolidine instead of D-serine) to the oxazolomycin right-hand side.
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Semak, Vladislav. "Synthesis of 1S-ethyl-4-substituted quinolizidines and other potentially bioactive compounds." Doctoral thesis, Universitat de Barcelona, 2012. http://hdl.handle.net/10803/97241.

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Esta Tesis Doctoral se presenta como Compendio de publicaciones. Los capítulos en los que se ha dividido la presente Tesis son los siguientes: Capítulo 1 – parte A: Enantioselective, Protecting Group-Free Synthesis of 1S-Ethyl-4-Substituted Quinolizidines Se ha descrito una síntesis enantioselectiva que no implica grupos protectores para acceder a la quinolizidina clave 6 a partir de la lactama bicíclica derivada de fenilglicinol 1. La adición de un reactivo organometálico a 6 ocurre de manera estereoselectiva para conducir a las quinolizidinas 1S-etil-4-sustituidas 4-epi-207I y 7-9. Siguiendo una secuencia sintética análoga, se preparó el compuesto 9a-epi-6. Sin embargo, la adición de reactivos de Grignard al compuesto 9a-epi-6 no ocurre de manera estereoselectiva. Capítulo 1 – parte B: A practical procedure for the removal of the phenylethanol moiety from phenylglycinol-derived lactams Las lactamas bicíclicas no racémicas derivadas de fenilglicinol se han relevado como intermedios clave en la preparación de compuestos nitrogenados enantiopuros. En este capítulo se describe la eliminación del inductor quiral de piperidonas sustituidas utilizando aire u oxígeno en medio básico. Capítulo 2: Synthesis of triheptanoin and formulation as a solid diet for rodents En el presente estudio se describe la síntesis eficaz de triheptanoina de elevada pureza a partir de glicerol y ácido heptanoico, en presencia de carbono sulfonado como catalizador. La triheptanoina se formula como un sólido estable para que constituya la base de una dieta cetogénica mediante la combinación de custro gentes de formulación comerciales; dos tipos de sílica, celulosa microcristalina y talco. La adecuación de la dieta se prueba en ratones C57BI/6 en un periodo de 15 días, comparando el estado general y el cambio de peso corporal. Capítulo 3: Toluene dioxygenase (TDO) mediated oxidation of halogen-substituted benzoate esters Una serie de esteres benzoicos metílicos sustituidos en o-, m- y p- se han sometido a hidroxilación enzimática via fermetación con E. coli JM109 8pDTG601A). Solo se metabolizaron los benzoatos sustituidos en orto. El 2-fluorobenzoato de metilo produjo regioselectivamente solo un diol mientras que el 2-cloro, 2-bromo y 2-iodobenzoato de metilo proporciona una mezcla de regioisómeros. Capítulo 4: Dauben–Michno oxidative transposition of allylic cyanohydrins Enantiomeric switch of (–)-carvone to (+)-carvone Cuando cianohidrinas alílicas se someten a la reacción de oxidación de Dauben-Michno a bajas temperaturas se accede a β-cianoenonas en buenos a excelentes rendimientos. El potencial de esta trasposición oxidativa se pone de manifiesto en enonas que contienen un plano latente de simetría como por ejemplo la conversión de la (-)-carvona en su enantiomero.
A dissertation submitted by Vladislav SEMAK to obtain a doctoral degree from University of Barcelona. This thesis was developed under the supervision of Dr. Carmen Escolano Mirón from Faculty of Pharmacy, University of Barcelona. This doctoral thesis is presented as a compendium of publications. The thesis is divided in four chapters: CHAPTER 1 – PART A: Enantioselective, Protecting Group-Free Synthesis of 1S-Ethyl-4-Substituted Quinolizidines (Amat, M.; Semak, V.; Escolano, C.; Molins, E.; Bosch, J. Org. Biomol. Chem. 2012, 10, 6866-6875.) A practical enantioselective protecting group-free four-step route to the key quinolizidinone 6 from phenylglycinol-derived bicyclic lactam 1 is reported. The organometallic addition reaction upon 6 takes place stereoselectively to give 1-ethyl-4-substituted quinolizidines 4-epi-207I and 7-9. Following a similar synthetic sequence, 9a-epi-6 is also accessed. However, the addition of Grignard reagents upon 9a-epi-6 proceeds in a non-stereoselective manner. In order to gain insight into the different stereochemical outcome in the two series, theoretical calculations on the iminium salts A and B have been performed. The study concludes that the addition of the hydride, which is the step that determines the configuration of the final products, occurs in a stereoelectronic controlled manner. CHAPTER 1 – PART B: A practical procedure for the removal of the phenylethanol moiety from phenylglycinol-derived lactams (V. Semak; C, Escolano; C. Arróniz; J. Bosch; M. Amat Tetrahedron: Asymmetry 2010, 21, 2542-2549.) Chiral non-racemic bicyclic lactams derived from phenylglycinol have been appointed as key building blocks for the preparation of enantiopure nitrogen compounds. The removal of the chiral inductor leading to substituted piperidones by using air or oxygen in basic media is presented in this chapter. CHAPTER 2: Synthesis of triheptanoin and formulation as a solid diet for rodents (Semak, V.; Semakova, J.; Halbaut, L.; Asó, E.; Ferrer, I.; Calpena, A.; Escolano, C.; Perales, J. C. Eur. J. Lipid Sci. Technol. 2012, 114, 889-895.) In the present study, we successfully synthesized triheptanoin to the highest standards of purity from glycerol and heptanoic acid, using sulfonated charcoal as a catalyst. Triheptanoin oil was then formulated as a solid, stable and palatable preparation using a ketogenic base and a combination of four commercially available formulation agents: hydrophilic fumed silica, hydrophobic fumed silica, microcrystalline cellulose, and talc. Diet compliance and safety was tested on C57Bl/6 mice over a 15-week period, comparing overall status and body weight change. CHAPTER 3: Toluene dioxygenase mediated oxidation of halogen-substituted benzoate esters (Semak, V.; Metcalf, T. A.; Endoma-Arias, M. A. A.; Mach, P.; Hudlicky, T. Org. Biomol. Chem. 2012, 10, 4407-4416.) A series of ortho-, meta-, and para-halogen-substituted methyl benzoate esters was subjected to enzymatic dihydroxylation via the whole-cell fermentation with E. coli JM109 (pDTG601A). Only ortho-substituted benzoates were metabolized. Methyl 2-fluorobenzoate yielded one diol regioselectively whereas methyl 2-chloro-, methyl 2-bromo- and methyl 2-iodobenzoates each yielded a mixture of regioisomers. Absolute stereochemistry was determined for all new metabolites. Computational analysis of these results and a possible rationale for the regioselectivity of the enzymatic dihydroxylation is advanced. CHAPTER 4: Dauben–Michno oxidative transposition of allylic cyanohydrins. Enantiomeric switch of (–)-carvone to (+)-carvone. (Hudlicky, J. R.; Werner, L.; Semak, V.; Simionescu, R.; Hudlicky, T. Can. J. Chem. 2011, 89, 535-543.) Allylic cyanohydrins were subjected to Dauben–Michno oxidation at low temperatures to provide β-cyanoenones in good to excellent yields. The potential of this oxidative transposition as a means of an enantiomeric switch of enones containing a latent plane of symmetry was tested by conversion of (–)-carvone to its enantiomer.
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Silva, Franck. "Synthesis and reactivity of enantioenriched β-hydroxyenones and -ynones." Thesis, University of Oxford, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.670096.

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Kilburn, John Paul. "Novel solid-phase synthesis strategies for the preparation of heterocycles and guanidines." Thesis, Open University, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.247056.

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Li, Sifeng. "Hydrofunctionalization of alkenes and their applications in the synthesis of bioactive compounds." HKBU Institutional Repository, 2020. https://repository.hkbu.edu.hk/etd_oa/812.

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Heterocycles are privileged structural motifs found in many natural products and biologically active compounds. Given the prevalence of this structural unit, there has been considerable interest and challenge in developing methods for construction optically pure heterocycles in organic synthesis and pharmaceutical chemistry. The skeleton of hydronaphthalene and indole are pervasive structural motifs in the pharmaceutical drugs that exhibit various bioactivities. This dissertation is mainly focused on the development of transition-metal-catalyzed asymmetric functionalization of alkenes, including the hydroselenation and hydroamination of various oxa/azabicyclic olefins for the synthesis of bioactive compounds and structural modification of oleanolic acid. An efficient rhodium catalytic system consisting of Rh(COD)2OTf/(S)-xyl-Binap, and n-Bu4NI was developed for the asymmetric hydroselenation of various oxa/azabicyclic olefins with diaryl diselenides instead of the unstable, malodorous selenol compounds. Under these reaction conditions, a wide range of heterobicyclic alkenes produced selenol containing hydronaphthalene derivatives in high yields (up to 96%) along with excellent enantioselectivities (up to 97%), overcoming the self- promoted racemic hydroselenation. The exo-configuration of the exclusive addition product was confirmed by X-ray crystal structure analysis. The strategy has also been applied to the kinetic resolution of unsymmetric oxabenzonorbornadiene. Further, these selenium compounds can catalyze the oxidative coupling reaction of 2-naphthols. Then, for the synthesis of trans 1-indolyl dihydronaphthalenols, a highly enantioselective Rh/Pd dual-metal sequentially catalytic system was revealed through intermolecular and intramolecular cascade hydroamination in the reaction of oxabenzonorbornadienes with 2-alkynylanilines. The exclusive trans-configuration of 1-(2-phenyl)indolyl dihydronaphthalenol was identified by X-ray crystal analysis. Various substituents, such as aryl, heteroaryl, alkyl, and silyl groups on alkynyl starting material can be used as compatible nucleophiles in the reaction to give excellent iii enantiomeric excesses (up to 99%) with good yields (up to 88%) under mild conditions. The reaction can be performed on a gram scale, while the indole derivatives could be transformed at the hydroxyl and indolyl funtionalities. The in silico and in vitro screening showed that the novel 1-indolyl dihydronaphthalenol products can serve as potential lead compounds for treating inflammation disease. At last, a series of functional groups, including carboxyl, phosphate, sulfone, triazole, tertiary amine, and glycosyl have been incorporated into oleanolic acid to improve its water solubility. A wide range of their derivatives have been obtained, and it was found that carboxyl salt, phosphate salt, and sulfonate salt contribute to the increase of the solubilities in water; up to 8 g/L was gained for carboxylate salt, which also provides the possibility to improve the bioavailability of these compounds
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Antonopoulou, Io. "Use of feruloyl esterases for chemoenzymatic synthesis of bioactive compounds." Licentiate thesis, Luleå tekniska universitet, Kemiteknik, 2017. http://urn.kb.se/resolve?urn=urn:nbn:se:ltu:diva-62836.

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Feruloyl esterases (FAEs, EC 3.1.1.73) represent a subclass of carboxylic acid esterases that under normal conditions catalyze the hydrolysis of the ester bond between hydroxycinnamic acids (ferulic acid, sinapic acid, caffeic acid, p-coumaric acid) and arabinose residues in plant cell walls. Based on their specificity towards monoferulates and diferulates, substitutions on the phenolic ring and on their amino acid sequence identity, they have been classified into four types (A-D). The use of FAEs as accessory enzymes for the degradation of lignocellulosic biomass and their synergism with other hemicellulases has been studied for application in many industries, such as the food, the biofuel and the paper pulp industry. In the recent years, the use of FAEs as biosynthetic tools has been underlined. Under low water content, these enzymes are able to catalyze the esterification of hydroxycinnamic acids or the transesterification of their esters resulting in compounds with altered lipophilicity, revealing a great potential for tailor-made modification of natural antioxidants for use in cosmetic, cosmeceutical and pharmaceutical industries. The first part of the thesis is focused on the optimization of reaction conditions for the synthesis of two bioactive esters: prenyl ferulate and L-arabinose ferulate using 5 FAEs (FaeA1, FaeA2, FaeB1, FaeB2 and MtFae1a) from Myceliophthora thermophila in detergentless microemulsions. Reaction conditions were optimized investigating parameters such as the medium composition, the substrate concentration, the enzyme load, the pH, the temperature and the agitation. Regarding the synthesis of prenyl ferulate, FaeB2 offered the highest transesterification yield (71.5±0.2%) after 24 h of incubation at 30oC using 60 mM vinyl ferulate (VFA), 1 M prenol and 0.02 mg FAE/mL in a mixture comprising of 53.4: 43.4: 3.2 v/v/v n-hexane: t-butanol: 100 mM MOPS-NaOH pH 6.0. At these conditions, the competitive hydrolysis was 4-7 fold minimized. Regarding the synthesis of L-arabinose ferulate, FaeA1 offered highest transesterification yield (35.9±2.96%) after 8 h of incubation at 50oC using 80 mM VFA, 55 mM L-arabinose and 0.02 mg FAE/mL in a mixture of 19.8: 74.7: 5.5 v/v/v n-hexane: t-butanol: 100 mM MOPS-NaOH pH 8.0. It was revealed that the type B FAEs from M. thermophila show higher preference to more lipophilic acceptors like prenol, while the type A FaeA1 was more efficient in the synthesis of the more hydrophilic L-arabinose ferulate. The second part of the thesis is focused on the investigation of the basis of the type A classification of a well-studied FAE from Aspergillus niger (AnFaeA) by comparing its activity towards methyl and arabinose hydroxycinnamate esters. For this purpose, L-arabinose ferulate and caffeate were synthesized enzymatically. kcat/Km ratios revealed that AnFaeA hydrolyzed arabinose ferulate 1600 times and arabinose caffeate 6.5 times more efficiently than methyl esters. This study demonstrated that short alkyl chain hydroxycinnamate esters which are used nowadays for FAE classification can lead to activity misclassification, while L-arabinose esters could potentially substitute synthetic esters in classification.
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Saito, Yu. "Synthesis of bioactive compounds: Synthetic study of D-Lac-terminated peptidoglycan fragment structures." Thesis, KTH, Kemiteknik, 2021. http://urn.kb.se/resolve?urn=urn:nbn:se:kth:diva-300085.

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Peptidoglycan (PGN) är en bakteriecellväggskomponent och känd för att känna igen olika receptorer eller enzymer för att leda aktiveringsimmunsystemet. Den allmänna strukturen för PGN består av sockerkedjor inklusive N-acetylglutamin (GlcNAc), N-acetylmuraminsyra (MurNAc) och tvärbundna peptidkedjor. PGN-fragment med D-Lac-ändpeptider har hittats från vankomycinresistenta enterokocker men ett kemiskt syntetiserat PGN-fragment med en D-Lac-ändpeptid har inte undersökts i detalj. Således fokuserade vi på syntesen av PGN-fragmentstrukturer som inkluderar en D-Ala-D-Lac-rest vid den terminala delen av peptidkedjan. För att syntetisera dessa fragmentstrukturer planerade vi att kombinera fastfassyntes (för Lac-peptiddelen) och lösningsfassyntes (för glykanberedning och kondensation). Detta tillvägagångssätt är fördelaktigt för framställning av peptidoglykanfragment med en komplex grenad peptiddel. Först beredde vi sockerdelen MurNAc-derivatet i lösningsfassyntes från ett glukosderivat. Medan den Lac-innehållande peptiden framställdes med fastfas-peptidsyntes med användning av 2-klortritylkloridharts. Med denna förening gav kondensationen av dessa två föreningar det önskade D-Lac-avslutade peptidoglykanfragmentet.
Peptidoglycan (PGN) is a bacterial cell wall component and known to be recognized by various receptors or enzymes to lead the activation immune system. The general structure of PGN consists of sugar chains including N-acetylglutamine (GlcNAc), N-acetylmuramic acid (MurNAc) and cross-linked peptide chains. PGN fragments having D-Lac terminus peptides have been found from vancomycin-resistant enterococcus, but a chemically synthesized PGN fragment having a D-Lac terminus peptide has not been examined in detail. Thus, we focused on the synthesis of PGN fragment structures that include a D-Ala-D-Lac residue at the terminal part of the peptide chain. In order to synthesize these fragment structures, we planned to combine solid-phase synthesis (for the peptide- Lac part) and solution-phase synthesis (for glycan preparation and the condensation). This approach is advantageous for the preparation of peptidoglycan fragments having complex branched peptide moiety. First, we prepared the sugar moiety MurNAc derivative in solution-phase synthesis from a glucose derivative. While, the Lac-containing peptide was prepared with solid-phase peptide synthesis using 2-chlorotrityl chloride resin. Having this compound, the condensation of these two compounds gave the desired D-Lac-terminated peptidoglycan fragment.
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Books on the topic "Bioactive compounds - Synthesis"

1

Chuanjun, Song, ed. Wu wei zi huo xing cheng fen ji hua xue he cheng: Bioactive ingredient of schisandra chinensis and their syntheses. Hefei Shi: Zhongguo ke xue ji shu da xue chu ban she, 2012.

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H, Waldmann, and Janning Petra, eds. Chemical biology: Learning through case studies. Weinheim: Wiley-VCH, 2009.

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Inuki, Shinsuke. Total Synthesis of Bioactive Natural Products by Palladium-Catalyzed Domino Cyclization of Allenes and Related Compounds. Tokyo: Springer Tokyo, 2012. http://dx.doi.org/10.1007/978-4-431-54043-4.

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Eich, Eckart. Solanaceae and convolvulaceae - secondary metabolites: Biosynthesis, chemotaxonomy, biological and economic significance : a handbook. Berlin: Springer, 2008.

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Biocatalytic Synthesis of Bioactive Compounds. MDPI, 2020. http://dx.doi.org/10.3390/books978-3-03943-572-2.

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Multicomponent Reactions: Synthesis of Bioactive Heterocycles. Taylor & Francis Group, 2017.

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Ameta, K. L., and Anshu Dandia. Multicomponent Reactions: Synthesis of Bioactive Heterocycles. Taylor & Francis Group, 2017.

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Ameta, K. L., and Anshu Dandia. Multicomponent Reactions: Synthesis of Bioactive Heterocycles. Taylor & Francis Group, 2017.

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Ameta, K. L., and Anshu Dandia. Multicomponent Reactions: Synthesis of Bioactive Heterocycles. Taylor & Francis Group, 2017.

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Ameta, K. L., and Anshu Dandia. Multicomponent Reactions: Synthesis of Bioactive Heterocycles. Taylor & Francis Group, 2017.

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Book chapters on the topic "Bioactive compounds - Synthesis"

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Ata, Athar, and Samina Naz. "Synthesis of Bioactive Heterocyclic Compounds." In Greener Synthesis of Organic Compounds, Drugs and Natural Products, 137–50. Boca Raton: CRC Press, 2022. http://dx.doi.org/10.1201/9781003089162-8.

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Phougat, Neetu, Manish Kumar, Reena V. Saini, and Anil Kumar Chhillar. "Green Chemistry Approach Towards Nanoparticle Synthesis." In Metabolic Engineering for Bioactive Compounds, 249–68. Singapore: Springer Singapore, 2017. http://dx.doi.org/10.1007/978-981-10-5511-9_12.

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Chênevert, R., R. Gagnon, M. Desjardins, M. Dickman, P. Bureau, G. Fortier, R. Martin, M. Létourneau, S. Thiboutot, and R. Bel-Rhlid. "Chemoenzymatic Synthesis of Natural Products and Bioactive Compounds." In Microbial Reagents in Organic Synthesis, 135–47. Dordrecht: Springer Netherlands, 1992. http://dx.doi.org/10.1007/978-94-011-2444-7_11.

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Kumari, Pooja, Sanjay Kumar, Anupam Patra, Baljinder Singh, Vimal Pandey, and Sahil Mehta. "Plant-Microbe Symbiosis led synthesis of Bioactive Compounds." In Antioxidants in Plant-Microbe Interaction, 21–40. Singapore: Springer Singapore, 2021. http://dx.doi.org/10.1007/978-981-16-1350-0_2.

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Dandia, Anshu, Shyam L. Gupta, and Shuchi Maheshwari. "Molecular Iodine: Mild, Green, and Nontoxic Lewis Acid Catalyst for the Synthesis of Heterocyclic Compounds." In Green Chemistry: Synthesis of Bioactive Heterocycles, 277–327. New Delhi: Springer India, 2014. http://dx.doi.org/10.1007/978-81-322-1850-0_10.

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Thiengchanya, Adul, Charoen Eung, Nongluk Tanikkul, and Kan Chantrapromma. "Chemical Synthesis of Bioactive Polyamines from Solanaceous Plants." In Ciba Foundation Symposium 154 - Bioactive Compounds from Plants, 99–111. Chichester, UK: John Wiley & Sons, Ltd., 2007. http://dx.doi.org/10.1002/9780470514009.ch8.

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Fox, Karen, Rafael Luque, Luiz Antonio Soares Romeiro, and Maria Laura Bolognesi. "New Biomass Reagents for the Synthesis of Bioactive Compounds." In Topics in Medicinal Chemistry, 373–89. Cham: Springer International Publishing, 2021. http://dx.doi.org/10.1007/7355_2021_118.

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Slomkowski, S., S. Sosnowski, M. Gadzinowski, C. Pichot, and A. Elaissari. "Direct Synthesis of Polyester Microspheres, Potential Carriers of Bioactive Compounds." In ACS Symposium Series, 143–53. Washington, DC: American Chemical Society, 1998. http://dx.doi.org/10.1021/bk-1998-0709.ch011.

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Ho, Thanh C., and Marcus A. Tius. "Synthesis of Classical/Nonclassical Hybrid Cannabinoids and Related Compounds." In Cutting-Edge Organic Synthesis and Chemical Biology of Bioactive Molecules, 247–89. Singapore: Springer Singapore, 2019. http://dx.doi.org/10.1007/978-981-13-6244-6_11.

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Ley, Steven V. "Synthesis of Antifeedants for Insects: Novel Behaviour-Modifying Chemicals from Plants." In Ciba Foundation Symposium 154 - Bioactive Compounds from Plants, 80–98. Chichester, UK: John Wiley & Sons, Ltd., 2007. http://dx.doi.org/10.1002/9780470514009.ch7.

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Conference papers on the topic "Bioactive compounds - Synthesis"

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Barbosa, Flavio A. R., Rômulo F. S. Canto, and Antonio L. Braga. "Synthesis of novel 6-seleno-dihydropyrimidinones: Potentially bioactive compounds." In 15th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-bmos2013_2013819222620.

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Ferreira, Samuel R. A., Jesus M. Pena, Simone C. Silva, and Giuliano C. Clososki. "Directed Functionalization of Quinoxalines Aiming the Synthesis of Bioactive Compounds." In 15th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-bmos2013_201391317050.

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Tulaidan, Halyna, Ruslan Symchak, and Vitaliy Вaranovskyi. "APPLICATION OF ANIONARYLATION REACTION FOR SYNTHESIS OF BIOACTIVE COMPOUNDS." In SCIENTIFIC PRACTICE: MODERN AND CLASSICAL RESEARCH METHODS. European Scientific Platform, 2022. http://dx.doi.org/10.36074/logos-16.09.2022.20.

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Birichevskaya, L. L., M. A. Vinter, A. A. Doroshevich, M. А. Khancheuski, E. I. Kvasyuk, and A. I. Zinchenko. "SYNTHESIS OF THE MODIFIED NUCLEOSIDE 8-BROMADENOSINE AND ITS PHOSPHOLIPID DERIVATIVE." In SAKHAROV READINGS 2021: ENVIRONMENTAL PROBLEMS OF THE XXI CENTURY. International Sakharov Environmental Institute of Belarusian State University, 2021. http://dx.doi.org/10.46646/sakh-2021-2-20-23.

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Modified nucleoside 8-bromoadenosine possessing high reactive capacity may serve as a basic compound for the synthesis of a large number of purine antimetabolites showing potentially therapeutic activities toward several tumor and viral diseases. In this study, 8-bromoadenosine was produced by a simple eco-friendly procedure following the treatment of nucleoside precursor adenosine with aqueous bromine solution. In the course of enzymatic transphosphatidylation reaction, the first synthesis of phospholipid derivative of the above-mentioned nucleoside -5‘-(1,2-dimyristoyl phosphatidyl)-8-bromoadenosine was accomplished. Novel compounds may presumably act as non-toxic progenitors of bioactive antimetabolites to be used in drug formulas.
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Sousa, Emília, Agostinho Lemos, Ana Gomes, Sara Cravo, and Madalena Pinto. "Synthesis of Aminated Xanthones: Exploiting Chemical Routes to Reach for Bioactive Compounds." In 1st International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecmc-1-a022.

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Nilsson, Johan, Thomas Szabo, Gaston Lavén, Martin Kullberg, Adam Kraszewski, and Jacek Stawinski. "Developing synthetic methods for bioactive phosphorus compounds. A progress report." In XIIIth Symposium on Chemistry of Nucleic Acid Components. Prague: Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 2005. http://dx.doi.org/10.1135/css200507189.

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Guardado, Estela, Maria Matos, Lourdes Santana, Eugenio Uriarte, and Enrique Molina. "Influence of thermodynamic parameters on the genotoxicity of bioactive phenolic compounds present in food." In The 17th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2013. http://dx.doi.org/10.3390/ecsoc-17-e013.

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Lukasiewicz, Marcin, Magdalena Malysa-Pasko, Piotr Jakubowski, and Magdalena Kulig. "APPLICATION OF COMMERCIAL WHEY PROTEINS FOR EXTRACTION OF BIOACTIVE COMPOUNDS FROM ELDERBERRY." In The 21st International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2017. http://dx.doi.org/10.3390/ecsoc-21-04738.

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Malysa-Pasko, Magdalena, Marcin Lukasiewicz, and Piotr Jakubowski. "MICROWAVE-ASSISTED EXTRACTION OF BIOACTIVE COMPOUNDS FROM SEEDS OF MILK THISTLE, BLACK CUMIN AND CORIANDER." In The 19th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecsoc-19-b005.

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