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 41 for “"Peptidomimetics"”.
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Design and synthesis and testing of conformationally constrained peptidomimetics.
… describes the design, synthesis and testing of peptidomimetics pre-organised into bioactive conformations. Chapter One introduces the concept of peptidomimetics, their importance as potential pharmaceuticals. The concept of constraining a compound into a bioactive conformation (α-helix, β-turn …
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Syntheses, bioactivities and conformations of peptidomimetics containing 2,3-methanoamino acids
… -2-oxo-3-oxa-bicyclo (3.1.0) hexane. Peptidomimetics containing some of these 2,3-methanoamino acids mentioned above were synthesized via a solid phase approach. The Met$\sp2$ in neuropeptide Phe-Met-Arg-Phe-NH$\sb2$ (FMRF-NH$\sb2$, one letter code for amino acids) was systematically …
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Synthesis of Novel Chiral Heterocyclic Compounds for Antibacterial Agents and Peptidomimetics
Small chiral molecules are very important building blocks in the synthesis of biologically active compounds. These building blocks include nitrogen and oxygen-containing heterocycles such as 2-oxazolidinones, 1,3-oxazinan-2-ones, 2-oxazolines, oxazines, morpholine and morpholinones. Because of …
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Synthesis of Novel Amino Acids and Peptidomimetics as Tools for Drug Discovery
… describes the synthesis of novel amino acids and peptidomimetics for use as tools for drug discovery. The first part of this study focuses on the preparation of modified tyrosine analogues using metal-catalysed coupling reactions and the incorporation of these novel amino acid building blocks into …
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DESIGN AND SYNTHESIS OF NEW PEPTIDOMIMETICS AS POTENTIAL INHIBITORS OF HIV-1 PROTEASE
… with the design and synthesis of peptides and peptidomimetics as potential inhibitors of HIV-1 protease that can circumvent drug resistance and that can be alternatives to active site PR inhibitors. Two different approaches were applied to reach our target. The first one, described in chapter …
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Design, synthesis and mode of action of short biphenyl and anthranilamide cationic peptidomimetics
… focused on the development of short cationic peptidomimetics that employ 3'-amino-[1, 1 '-biphenyl)-3-carboxylic acid and anthranilic acid backbones segregated by hydrophobic and cationic groups. The biphenyl peptidomimetic compounds showed that simple diaminoethanes and their respective …
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COMPUTATIONAL DESIGN OF PEPTIDES AND PEPTIDOMIMETICS AS POTENTIAL THERAPEUTIC AGENTS TO SATISFY PRESSING MEDICAL NEEDS
… effects of the peptides by designing peptidomimetics, which do not contain the fleeting amide bonds. In this research project, I have applied advanced computational approaches in combination with biochemical and biophysical analysis, to different case studies, in order to discover, …
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Antiviral Agents: 3,5-Disubstituted 1,2,4-Oxadiazole Derivatives and Novel Peptidomimetics Containing Hydroxyethyl Isostere and Imidazolidinone Structures
… those mechanisms in order to treat diseases. Peptidomimetics are compounds with behavior similar to that of the peptide they mimic, but typically have structural enhancements that prevent quick metabolism or excretion from the system.</p> <p>A new class of peptidomimetics derived from both …
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Synthesis of non-natural amino acids, peptidomimetics, and electrochemical characterization of the structures obtained by self-assembly
L'uso di amminoacidi (AA) non naturali, tra i quali i β-AA, per la sintesi di peptidomimetici riscuote sempre più interesse, poiché si tratta di sequenze con la stessa attività biologica dei peptidi naturali ma con una maggiore stabilità proteolitica e conformazionale. Inoltre, la capacità dei …
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Design and stereoselective synthesis of novel bicyclicbeta-turn dipeptide mimetics and cis-4-substitutedproline analogues for peptides and peptidomimetics
… some strategies have been developed to prepare peptidomimetics with constrained conformations. Both local conformational constraints and global conformational constraints can provide important insights into the structural and topographical basis of biological activity. A series of novel …
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Design, Syntheses, and Bioactivities of Conformationally Locked Pin1 Ground State Inhibitors
… same starting material. Conformationally locked peptidomimetics, including two exactly matched peptidomimetics, Ac–Phe–Phe–pSer–Ψ(<i>E</i>)CH=C]Pro–Arg–NH2 and Ac–Phe–Phe–pSer–Ψ[(<i>Z</i>)CH=C]Pro–Arg–NH2, were synthesized from these Ser-Pro isosteres using Fmoc SPPS. A protocol for in vitro Pin1 …
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USING B-STRAND AND B-HAIRPIN PEPTIDOMIMETICS INDUCED BY CONSTRAINED AMINO ACIDS TO MODULATE THE AGGREGATION OF THE MICROTUBULE ASSOCIATED PROTEIN TAU: DESIGN, SYNTHESIS AND EVALUATION
… for the first time, the possibility of creating peptidomimetics capable of stabilizing either a β-hairpin or an extended structure to modulate Tau protein aggregation. This work focuses on three distinct peptidomimetic units with the goal of highlighting the significant role of secondary …
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I The tandem chain extension-acylation reaction II Synthesis of papyracillic acid A: Application of the tandem homologation-acylation reaction III Synthesis of tetrahydrofuran-based peptidomimetics
… for the synthesis of tetrahydrofuran-based peptidomimetics. A variety of amino acid derived beta-keto imides and aldehydes were used during the initial tandem homologation-aldol reaction. High diastereocontrol was achieved during reductive cyclization when a cis relationship was present …
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Interaction of peptides, peptidomimetics and other drug candidates with the DI/tripeptide transport system in intestinal epithelial cells, using the in vitro caco-2 cell culture system
An uptake system was developed using Caco-2 cell monolayers and the dipeptide, glycyl-[3H]L-proline, as a probe compound. Glycyl-[3H]L-proline uptake was via the di-/tripeptide transport system (DTS) and, exhibited concentration-, pH- and temperature-dependency. Dipeptides inhibited uptake of the …
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INTEGRIN ALPHAVBETA3 AS THERAPEUTIC TARGET AND IMAGING BIOMARKER FOR VASCULAR ENDOTHELIAL CELLS AND CANCER EPITHELIAL CELLS
… antagonists comprise synthetic peptides and peptidomimetics. Synthetic peptides mimic the structure of natural integrin binding ligands. The largest class of synthetic peptides so far developed comprises RGD peptides, given that the RGD sequence is commonly found in several glycoproteins of …
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Part 1 Design, Synthesis and Bioactivity of a Phosphorylated Prodrug for the Inhibition of Pin1; Part 2 Conformational Specificity of Cdc25c Substrate for Cdc2 Kinase using LC-MS/MS
… Ser-Ψ[(E)CH=C]-Pro-OH were incorporated into two peptidomimetics derived from human Cdc25c. Phosphorylation of these two peptidomimetics by the incubation with Cdc2 was studied using LC-MS/MS technique. It was found that Cdc2 kinase was conformationally specific to its Cdc25c substrate. Only the …
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Thermodynamic and Structural Characterization of the Interaction between Wd40 Repeat Containing Protein 5 (Wdr5) and Human Set1 Family Methyltransferases
… analysis further to identify other peptidomimetics by characterizing peptides identified in a randomized phage display screen, which are also highly specific inhibitors of MLL1 core complex. Crystal structures of these peptidomimetics reveal novel protein structural features that …
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New paradigm for drug design: Design and synthesis of novel biologically active peptides that are agonists at opioid receptors and antagonists at cholecystokinin receptors
… pain, a series of linear and cyclic peptides and peptidomimetics were designed based on the overlapping pharmacophores of opioid and CCK ligands. The CCK/opioid analogues were synthesized and evaluated for their biological activities. Several of the CCK/opioid analogues were found to …
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Submonomer Synthesis and Structure-activity Relationship Studies of Azapeptide Inhibitors of the Insulin Receptor Tyrosine Kinase
<p>Azapeptides are a class of peptide mimics (peptidomimetics), which have served as valuable tools for the development of peptide based therapeutic agents. The therapeutic promise of azapeptides has been correlated to its primary sequence modification which translates into bio-active secondary …
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Role of N-terminal residues of CCL19 and CCL21 in binding and activation of CCR7
… short (three to seven amino acids) peptides and peptidomimetics inspired by the seven N-terminal amino acid residues of CCL19 and CCL21 and pharmacologically characterised their ability to activate CCR7 or block the activation of CCR7 using a number of in vitro assays such as calcium flux, …
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