Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 37 for “"Tryptamine"”.
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A Modular Approach to Highly Functionalized Indole Derivatives and Syntheses of Tryptamine-based SHIP Inhibitors
… and intrinsic structural complexity. N-alkylated tryptamines, along with their analogs, are recognized as potent SHIP inhibitors and are considered privileged structures due their binding properties and diverse biological targeting. Also, the pyrrolo[2,3-a]indoline frameworks have been recognized …
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A general entry to C7-borono indole derivatives
… It has been applied to indole, tryptophan, and tryptamine derivatives. Further functionalization to a C7 phenolic tryptamine derivative is also described.
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Substrate analogs to investigate alkaloid biosynthesis in Catharanthus roseus
… All terpene indole alkaloids are derived from tryptamine and secologanin, which are coupled to form strictosidine by the enzyme strictosidine synthase (STR). Analysis of the tryptamine substrate specificity of strictosidine synthase (STR) revealed a subset of tryptamine analogs which were …
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Synthesis of the Antimalarial Flindersial Alkaloids
… cyclization would form the flinderole framework. Tryptamine and 3-butyn-2-one undergo a vinylogous Pictet-Spengler reaction to give a β-carboline, which opens to a 2-enone tryptamine in the presence of base. A BINOL catalyzed enantioselective conjugate addition of a vinyl boronic acid to the …
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The Design, Synthesis, and Investigation into Small Molecule Modulators of the Src Homology 2 Domain-Containing Inositol 5’-Phosphatase (SHIP)
… report details the investigation into tryptamine-based pan-SHIP1/2 inhibitors, as well as studies into a newly discovered sulfonamide-based SHIP1 selective agonist. Attempts to modulate SHIP activity by means of small molecules led us to develop and synthesize various small molecule …
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Understanding and manipulating alkaloid biosynthesis
… RebH to preferentially install chlorine onto tryptamine, the direct indole precursor for the MIAs. After reengineering RebH, we then overexpressed the tryptamine-specific mutant RebH Y455W and flavin reductase RebF in C. roseus and observed the de novo biosynthesis of a chlorinated unnatural …
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Elucidating the Hydration of Biomolecules: An Experimental and Computational Approach
… 2O)n, M+(indole)m(H2O) n, and M+ (tryptamine)(H2O)n.
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Experimental and Theoretical Studies of Supercritical Fluid Behavior
… solubilities of two decarboxylated amino acids, tryptamine and histamine, in supercritical ammonia (supercritical in pressure only) at 50(DEGREES)C. Solubilities are obtained for the pure solids and mixtures of the solids in 1:1 mole ratio. The solubilities of the mixed solids are determined …
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Total synthesis and anticancer evaluation of all known communesin alkaloids and related complex derivatives
… the catalytic asymmetric halocyclization of tryptamine derivatives, a stereoselective sulfinimine allylation, and an efficient cyclotryptamine-C3a-sulfamate synthesis by either a new silver-promoted nucleophilic amination or a rhodium-catalyzed C-H amination protocol.
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On the Binding of N1-substituted Tryptamines at h5-HT6 Receptors
… N1-Alkylsulfonyl- 78, and N1-benzyl-substituted tryptamines 33 were synthesized and affinities compared with their corresponding N1-benzenesulfonyl-substituted counterparts 31 at h5-HT6 receptors. None of the alkylsulfonyl or benzyl analogs displayed and/or retained the affinity of the simple …
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The effects of pulsed static and oscillating magnetic fields on rat pineal serotonin N-acetyltransferase activity
… I/10th of a pineal gland was incubated with 12mM tryptamine. At the specified tryptamine concentration, SNAT activity increased as the concentration of Acetyl CoA increased. The enzyme efficiency, as determined from its Km (8.19x10⁻⁴M), and the level of activity exceeded those measured in other …
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FROM BATCH TO FLOW: RETHINK THE WAY OF DOING CHEMISTRY
… of benzoxaboroles, photochemical synthesis of tryptamines and a scale-up and tech transfer of a continuous production and use of an alkyl nitrite are presented. In the first chapter, it is provided a general introduction to the concept of flow chemistry, explaining the main instruments and …
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Pin1 Inhibitors: Towards Understanding the Enzymatic Mechanism
… was found to be Fmocâ pSerâ Ψ[CH2N]-Proâ tryptamine, which had an IC50 value of 6.3 µM. This represents a 4.5-fold better inhibition for Pin1 than a comparable cis-amide alkene isostere. The co-crystal structure of Acâ pSerâ Ψ[CH2N]-Proâ tryptamine bound to Pin1 was determined to 1.76 Ã …
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CONTINUOUS-FLOW STRATEGIES FOR THE PREPARATION OF ACTIVE PHARMACEUTICAL INGREDIENTS AND RELEVANT INTERMEDIATES
… metallaphotoredox catalysis for the synthesis of tryptamine derivatives, highlighting the potential of light-driven processes to access structurally complex motifs under mild conditions. The thesis further addresses one of the major limitations of flow chemistry, namely solid handling, through the …
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A Nonribosomal Peptide Pheromone Controls Male-Induced Female Sexual Development in Schistosoma mansoni
… (SmNRPS) and a pheromone metabolite β-alanyl-tryptamine (BATT) were discovered to firstly demonstrate the way a male parasite might signal his paired female. Using RNA sequencing, biochemistry assays and metabolomic analysis, we believe a male parasite starts to secret SmNRPS synthesized BATT …
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Part A: Investigation of a newly identified plant Hernandia didymantha Donn, synthesis of phenethyl cinnamide Part B: Selective removal of ascaridol from the essential oil of Chenopodium ambrosioides var ambrosioides Part C: Synthesis of canophyllol analogues
… major more polar component was shown to be the tryptamine derivative phenethyl cinnamide, 1. The structure identification was based on comparison of literature data and a two step synthesis (80%) from cinnamic acid and tryptamine. Part B. Chenopodium ambrosioides has been known for centuries as …
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Charge and temperature effects on biomolecule hydration: an experimental and computational investigation
… and hydrated sodium- and potassium-containing tryptamine, 2-amino-1-phenylethanol and ephedrine. In every case, there are significant differences between spectra obtained at different temperatures as well as those containing different metal ions. The argon tagging method, which was used to …
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Crystallization studies of Pictet-Spenglerases
… reaction is a Pictet-Spengler coupling between tryptamine and secologanin and produces the biosynthetic intermediate strictosidine, common to all monoterpene indole alkaloids. To better understand the structural features that impart binding selectivity, crystallization studies of this enzyme …
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Studies on the synthesis of bisindole Aspidosperma alkaloids
… of the characteristic pentacyclic core from tryptamine and secologanin is summarized. Some representative examples of total syntheses of Aspidosperma alkaloids are discussed. Synthetic strategies for the synthesis of bisindole members of the family are also examined. II. Total Synthesis of …
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