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Showing 1 to 13 of 13 for “"Thioamide"”.
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Cocrystallisation involving the thioamide, amide and imide functional groups
… of novel cocrystals that incorporated the thioamide, amide and imide functional groups. A particular emphasis was placed on the characterisation of these cocrystals by single crystal X-ray diffraction methods. In Chapter One a summary of the intermolecular interactions utilised in this work …
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Thioamides And Proteolysis: Examining The Effects And Applications Of A Single-Atom Substitution
Thioamide substitution in the peptide backbone enables several applications in studying proteolysis, monitoring protease activity and in selective protease inhibition. To date, we have used model substrates to investigate the positional effects that these thioamide substitutions have on proteolysis …
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Chemical Modification Methods for Protein Misfolding Studies
… tools. Our group previously demonstrated that a thioamide, a single atom substitution of the peptide bond, could serve as a minimalist fluorescence quencher. In the current study, we showed the development of protein semi-synthesis strategies for the incorporation of thioamides into full-length …
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Functional and mechanistic elucidation of peptide backbone thioamidation
… YcaO enzymes can also install lactamidines and thioamides onto peptides through similar mechanisms. These modifications are found in a class of natural products named ribosomally synthesized and post-translationally modified peptides (RiPPs) and are critical for their biological functions. In …
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Experimental (spectroscopic) and theoretical studies of rhodanine (2-Thio-4-Oxothiazolidine) and its derivatives
… and 3-methylrodanine-containing both amide and thioamide moieties have been investigated from both an experimental and theoretical perspective. Experimental Raman (?o = 632.8 nm) and infrared spectra of the three compounds have been recorded in the solid state (protonated and deuteriated). …
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Total Syntheses of 1,2,4-Thiadiazole Natural Products
… prepared through the oxidative dimerisation of thioamide (±)-388. A selective dehydration of insatindigothiadiazoles A-D (33a-d) furnished diene (±)-31 which underwent regioselective thio-Diels-Alder reaction with 3-thioisatin 32 to form natural products 24a and 24b, along with diastereomer …
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Oxidative additions of amides to an iridium(I) metal center
… or an N-substituent. The attempts to form the thioamide analogues of the acetamide and benzamide complexes failed to produce stable iridium hydrides. Thioacetamide will add to [(COD)Ir(PMe3)3]CI in chloroform or methylene chloride; however~ any hydrido species which formed subsequently reacted …
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Small-molecule approaches to interrogate the druggability of the VHL E3 Cullin RING Ubiquitin Ligase
… signalling pathway. Additionally, a series of thioamide containing analogues of VH298 were designed to probe the hydroxyproline recognition of VHL ligands. On the second VHL pocket starting from a weak-affinity fragment hit (Kd > 1 mM) I performed iterative cycles of synthesis, biophysical …
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Elucidation and control of substrate recognition during RiPP biosynthesis
… nucleophiles and partner proteins to generate thioamide, macroamidine, and possibly other peptide posttranslational modifications. In Chapter 1, I comprehensively review the biosynthetic gene clusters (BGCs), natural products, functions, mechanisms, and applications of YcaO proteins and outline …
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Single-Payload Bioconjugation to Native Antibodies And A General Method for the Self-Immolative Release of Amide-Containing Molecules
… of the method for sulphonamides. Urea and thioamide release was also attempted but proved synthetically challenging. The utility of amide release was demonstrated by its successful application in the targeted release of linezolid from a prodrug using the cathepsin-cleavable dipeptide …
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Post-translational modifications catalyzed by RiPP and RiPP-adjacent enzymes
Ribosomally synthesized and post-translationally modified peptides (RiPPs) are, as their name suggests, constructed from ribosomal peptides. The scope of biosynthetic reactions utilized by Nature to transform these peptides into structurally fascinating natural products is astounding. Leveraging …