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 14 of 14 for “"Tetrahydroisoquinoline"”.
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Tetrahydroisoquinoline Neurotoxins in Parkinson Disease
… was to (1) determine the distribution of several tetrahydroisoquinoline (TIQ) derivatives in rodent, normal human and Parkinson disease (PD) brain, (2) quantify the levels of these TIQ derivatives in common food sources in an effort to link specific food intake patterns with the development of PD …
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Biosynthesis of tetrahydroisoquinoline scaffolds in yeast
… Saccharomyces cerevisiae was used to produce the tetrahydroisoquinoline alkaloid precursor (S)-norcoclaurine via a combination of yeast Ehrlich pathway metabolism of ʟ-tyrosine and expression of norcoclaurine synthase with a dopamine production pathway. Building on this, I developed a …
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Preclinical Study of Potential Antiglioma Novel Tetrahydroisoquinoline Analogs: Pharmacokinetics and Mechanism of Action
… are urgently needed.</p> <p>A novel series of tetrahydroisoquinoline derivatives with antiglioma activity has been undergoing drug metabolism/pharmacokinetics (DMPK)-guided lead optimization. EDL-291 was result from structure modification of last generation compound EDL-155. Its preclinical …
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SYNTHESIS, BIOLOGICAL ACTIVITY AND CONFORMATIONAL ANALYSIS OF FRAGMENT ANALOGUES OF ALPHA-MELANOTROPIN (PEPTIDE, STRUCTURE-FUNCTION, PHENYLGLYCINE, NMR, TETRAHYDROISOQUINOLINE-3-CARBOXYLATE).
α-MSH (α-melanotropin) is a naturally occurring linear tridecapeptide (Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH₂) that is primarily known for its ability to stimulate integumental melanocytes and more recently has been implicated in a variety of physiological and neurological …
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MOLECULAR MODELING STUDIES OF HEPARIN AND HEPARIN MIMETICS BINDING TO COAGULATION PROTEINS
… virtual screening of 24576 molecules based on tetrahydroisoquinoline core scaffold resulted in 92 hits that were predicted to bind preferentially in the PBS of activated antithrombin with good affinity. The work resulted in a predicted pharmacophore consisting of a 5,6-disulfated bicyclic …
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Synthesis and Evaluation of Tetrahydroprotoberberines as Dopamine Receptor Ligands
… tetracyclic alkaloids that belong to the tetrahydroisoquinoline family. A wide range of biological activities are associated with the THPB scaffold. Noted examples of THPB alkaloids, (-)-stepholidine <strong>2.1 </strong>(SPD), (-)-tetrahydropalmatine <strong>2.2 </strong>(THP), …
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Chemical studies of metabolites from Pacific Ocean marine sponges and the starfish Dermasterias imbricata
… at Enewetak. The synthetic confirmation of the tetrahydroisoquinoline substructure of the starfish metabolite imbricatine (3) was accomplished using a Pictet-Spengler reaction to couple the starting materials 3-(3,5-dihydroxyphenyl) alanine methyl ester (143) and sodium 3-(4-benzyloxyphenyl) …
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Radical Approaches to Alangium and Mitragyna Alkaloids
… a robust and efficient synthesis of an allyl tetrahydroisoquinoline core (i and j) was developed, following conversion into the desired radical precursors these compounds were treated with tributyltin hydride and a radical initiator. Finally, Chapter 4 investigates the radical cyclisation of …
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Enhancing the cooperative binding properties of1,1'-bis(1,2,3,4-tetrahydroisoquinolines)
… crown-6)ethanoyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline] could be controlled by the simultaneous coordination of the termini of the diperchlorate salt of 1,3-diaminopropane to the crown ether moieties of the ligand. A range of new N-substituted bisisoquinolines have been …
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Designing Direct and Indirect Factor Xa Inhibitors
… a focused library of tetrasulfated N–arylacyl tetrahydroisoquinoline (THIQ) nonsaccharide allosteric antithrombin activators was designed, synthesized, and biochemically evaluated to establish their structure–activity relationship (SAR). An N–arylacyl THIQ analog having carboxylate at …
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Glioma: A Tale of Corticosteroids, Thiopurines and Proposed Novel AntiGlioma Small Molecules
… activity of 2 classes of novel small molecules; tetrahydroisoquinoline (THIQ) and chromenes. These molecules were screened in vitro to find the most potent anticancer derivatives that exhibited the least toxicity on normal stromal cells. EDL-360 (5-10 µM) and SP-6-27 (IC50 = 7-21 nM) were the …
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Exploration of [2+2+2] cyclotrimerisation reactions of alkynes. A new methodology for the synthesis of small molecules to probe biological systems
The generation of new chemical entities (NCEs) for use in chemical biology and drug discovery is of wide interest to both academia and the pharmaceutical industry. In order to generate NCEs, this project focused on development of new synthetic methodologies using transition-metal mediated [2+2+2] …
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Exploration of [2+2+2] cyclotrimerisation reactions of alkynes. A new methodology for the synthesis of small molecules to probe biological systems
The generation of new chemical entities (NCEs) for use in chemical biology and drug discovery is of wide interest to both academia and the pharmaceutical industry. In order to generate NCEs, this project focused on development of new synthetic methodologies using transition-metal mediated [2+2+2] …