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 16 of 16 for “"tropane"”.
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TROPANE ALKALOID PRODUCTION BY DATURA
… cultures produced appreciable amounts of tropane alkaloids (<lug/gDW). Root cultures were far more productive (about 1000 ug/gDW total alkaloids). It was shown that the Increase in tropane alkaloid biosynthesis in cultured roots ran parallel with root elongation. Possible explanations for …
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Synthesis and Biological Evaluation of Novel GBR 12909 Tropane and Azetidine Hybrid Analogues
… 3-[2- (diarylmethoxyethyidenyl)]-N-substituted tropane derivatives were synthesized and the binding affinities of these compounds were determined at the dopamine (DAT), serotonin (SERT) and norepinephrine (NET) transporters in rat brain tissue preparations. The tropane derivatives were found to …
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Synthesis And Evaluation Of Novel Tropane Compounds As Potential Therapeutics For Drug Abuse
… affinities. These unique 3ƒÀ-aryl-3ƒ¿-arylmethoxytropane analogues incorporated the structure of dopamine selective 2-substituted-3-phenyltropanes and the design of serotonin selective meperidine derivatives. In general, the 3ƒÀ-aryl-3ƒ¿-arylmethoxytropane analogues exhibited greater potency for …
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Asymmetric Synthesis of Homotropinone and Tropane Alkaloids using Enantiopure Sulfinimines and the Synthesis and Applications of Methanoprolines
… the asymmetric synthesis of homotropinone and tropane alkaloids using enantiopure sulfinimines [RS(O)N=CR1R²] is the primary objective of this thesis. In one study a four-step intramolecular Mannich cyclization cascade reaction was devised for the asymmetric synthesis of substituted …
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Structural Determinants for Substrate and Inhibitor Recognition by the Dopamine Transporter
… of this pharmacophore- the positively charged tropane nitrogen atom, the seven-carbon tropane ring itself, and the aromatic substituent at the tropane C-3 position- were assessed for binding affinity and dopamine uptake inhibition at the same D79 DAT mutants. Only inhibitors with modifications …
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Development of Receptor-Targeted Imaging Agents: Integrated Gallium Complexes and Conjugated Cyclopentadienyl Tricarbonyl Rhenium and Technetium Complexes
… 99mTc, the development of 99mTc-labeled phenyl-tropane analogs with high affinity for the dopamine transporter (DAT) would provide a useful tool for imaging disorders in this transporter system, such as clinical diagnosis of Parkinson's disease. The Direct Double Ligand Transfer (DLT) reaction …
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Asymmetric Synthesis of 1,3-Amino Alcohols and Tropinone Derivatives From Enantiopure Sulfinimines
… nitrogen, such as piperidine, pyrrolidine and tropane, are widespread as natural product alkaloids and serve as templates for many bioactive drugs and drug candidates. The intent of this research is to the develop asymmetric syntheses of piperidine-containing syn and anti 1,3-amino alcohols as …
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Total synthesis of ferrugine and synthetic studies towards ferrugine and stemofoline
Tropane alkaloids, containing the 8-azabicyclo[3.2.1]octane ring system, are widespread in Nature. This thesis describes the total synthesis of the tropane alkaloid ferrugine, isolated from the arboreal species Darlingiana ferruginea and attempted synthesis of ferruginine, isolated from the …
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Dopamine Transporter (DAT) and Metabotropic Glutamate Receptor 5 (MGLU5) Irreversible Probes for Identifying Anti-Psychostimulant Therapeutics
… two specific aims: 1) identification of non-tropane DAT inhibitor photoprobes suitable for DAT structure-function studies, and 2) identification of irreversible mGlu5 NAM ligands as chemical probes suitable for mGlu5 structure-function studies. Under the first aim, methylphenidate (MP) and …
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Dopamine Transporter (DAT), Nicotinic Acetylcholine Receptor (nAChR), and Metabotropic Glutamate Receptor 2 (mGlu2) Irreversible Probes For Identifying Anti-Psychostimulant Therapeutics
… three specific aims: 1.) Identification of non-tropane photoprobes based on pyrovalerone (PV) suitable for DAT structure-function studies, 2.) Identification of bupropion (BP)-based photoprobes suitable for DAT, and nAChR structure-function studies, and 3.) Identification of irreversible mGlu2 …
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Application of X-ray Diffraction Methods and Molecular Mechanics Simulations to Structure Determination and Cotton Fiber Analysis
… structure determination of ethylene glycol bis(tropane-3-carboxylate) is presented as an example of the use of modern single-crystal x-ray instrumentation including the use of coupled charged devices (CCDs) as detectors for accurate data collection and rapid elucidation of crystal structures. …
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Enantiodivergent chemoenzymatic synthesis of codeine
… N-demethylation and Nacylation of morphine and tropane alkaloids are presented. In addition, reactions of a menthol-based version of the Burgess reagent with epoxides are discussed. The synthetic utility of this novel chiral derivative of the Burgess reagent was demonstrated by an …
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Investigations into the molecular evolution of plant terpene, alkaloid, and urushiol biosynthetic enzymes
… enzyme families involved in either nicotine/tropane alkaloid biosynthesis (putrescine N-methyltransferase) or primary metabolism (spermidine synthase) by attempting to interconvert a spermidine synthase to encode putrescine N-methyltransferase activity based upon past patterns of natural …
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Studies on biological activities of Scottish plants.
… novel compounds hederacine A, hederacine B, two tropane alkaloids isolated from Glechoma hederacea, centcyamine and cis-centcyamine, two indole alkaloids from Centuarea cyanus. The other alkaloids isolated were moschamine, cis-moschamine and N-(p-coumaroyl)-serotonin were isolated from Centaurea …
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Monoamine Transporter Photoaffinity Ligands Based On Methylphenidate and Citalopram: Rational Design, Chemical Synthesis, and Biochemical Application
… three specific aims: 1) identification of non-tropane photoprobes based on MP suitable for DAT structure-function studies, 2) identification of photoprobes based on CIT and ( S )-CIT suitable for SERT structure-function studies, and 3) development of a tandem photoaffinity …
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Investigating disturbances of brain 5-HT systems by experimental MRI and SPECT neuroimaging
… [125I]βCIT (2β-carbomethoxy-3β-(4-iodophenyl)tropane), and a relatively novel SERT tracer, [123I]ADAM (2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine) were examined using micro-SPECT. The data demonstrate that DTI did not detect any changes in white matter organisation in …