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Showing 1 to 13 of 13 for “"Peptide coupling"”.
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The preparation of racemic and optically active beta-amino-acids and their utilisation in peptide formation.
… are being isolated from biologically active peptide antibiotics with increasing frequency nowadays. Recognition of the importance of these amino acids, has led to their incorporation into synthetic peptide analogues and into polymers. The main part of this thesis reports the successful …
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Development of novel nutrapharmaceuticals combining the anti-oxidant and anti-inflammatory properties of n-3 fatty acids with a nitric oxide donor: a potential new preventative strategy for heart disease.
… L-cysteine ethyl ester (compound 3)) and peptide coupling based reactions, and full characterisation has been achieved. The nitration stage of synthesis was achieved using tert-butyl nitrite and 'fuming' NO as the nitrating agents. Successful nitration was determined by MS analysis and by …
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Synthesis of Novel 5-Aryl 2’-Deoxyuridine and 2’-Deoxycytidine Analogues
… of the nucleobase via a Suzuki-Miyaura cross-coupling reaction, yielding 5-phenyl-2’-deoxyuridine (5-PdU). After that, modification of the obtained 5-PdU at the C4 position was performed with benzotriazole-1-yl-oxy-tris-(dimethylamino)-phosphonium hexafluorophosphate (BOP, a peptide-coupling …
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Ring-Opening of Aziridine -2 -Carboxamides by Carbohydrate C1-O Nucleophiles. Stereoselective Preparation of O-Linked Glycopeptides
A new method for the synthesis of O-linked glycopeptides is described. The method uses the carbohydrate C1-O nucleophilic ring-opening of aziridine-2-carboxamides to access the target O-linked glycopeptides. The synthesis of the alpha-GalNAc-Ser class of glycopeptides is emphasized and either the …
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Synthesis of 4-Azidocoumarins and Their Use in Copper-Catalyzed Azide-Alkyne Cycloaddition reactions
… coumarins by reaction with the peptide coupling agent (benzotriazol-1-yloxy)tris-(dimethylamino)phosphonium hexafluorophosphate (BOP), and 1,8-diazabicycloundec-7-ene (DBU) as the base, in tetrahydrofuran (THF) solvent. The 4-benzotriazolyloxy coumarins were converted to the …
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Preparation of arylphosphinic acid derivatives as building blocks for binding sites
… developed, which involves palladium catalyzed coupling of aryl iodides with methyl phosphinate. This procedure is compatible with various functional groups and proceeds in reasonable yields. Symmetrically substituted diarylphosphinates can be prepared using two equivalents of the aryl iodide. …
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Molecular Encapsulation in Kinetically Trapped, Hydrogen-Bonded Pyrogallolarene Hexamers
… with carboxylic acids on the lower rim. Peptide coupling to create an amide linkage has also been studied for use in attachment to polymers.</p>
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Total Synthesis of the Unique Pederin Family Member Psymberin & Chemical Studies Toward Saliniketal Family Members: Saliniketal a, Salinisporamycin and Rifsaliniketal
… and a stepwise Sonogashira coupling/cycloisomerization/reduction sequence to construct the dihydroisocoumarin unit. The total synthesis of psymberin and its analogs would provide sufficient material for mode-of-action and SAR studies. The fourth chapter describes the …
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Nanotechnology approaches for improvoved vasoactive intestinal peptide based-drug delivery systems
… order to improve the drug delivery of the neuropeptide vasoactive intestinal peptide (VIP). Two main questions have been addressed using VIP engineered NPs: 1. VIP functionalized gold NPs. In this case, VIP could act as a drug/diagnostic molecule for theranostic applications. 2. VIP …
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Trichloroacetimidates as Alkylating Reagents in C-N Bond Formation and Synthesis of Aminosteroid and Quinoline Inhibitors of Src Homology 2 Domain-Containing Inositol Phosphatase (SHIP)
… of key reactions in this sequence, including a peptide coupling reaction and oxidative cyclization, was performed. Investigation into completing the synthesis of kapakahine C is ongoing.</p> <p>The inhibition of the SH2-containing inositol 5’-phosphatase (SHIP) can modulate the dephosphorylation …
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Discovery, structural characterisation and targeted engineering of bioactive peptides from amphibian skin secretion
… are remarkable sources of novel bioactive peptides. Among these, the antimicrobial peptides (AMPs) have demonstrated an outstanding efficacy in killing microorganisms via a general membranolytic mechanism, which may offer a prospect of solving specific target driven antibiotic-resistance. …
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Oligomers of beta-L-arabinosides of hydroxyproline : synthesis of the carbohydrate epitope of the Art v 1 allergen
… the â-Ara-Hyp monomer respectively, after which peptide coupling of the two compounds was performed using HATU as coupling reagent to give the product, Boc-([â-L-Araf]Hyp)2-OAll, in 60% yield. Similar approaches were employed using a [2+1] or [1+2] fragment condensation strategy to produce the …
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Development of Immune Modulators Targeting Autoimmune Disorders and Pulmonary Injury: Design, Synthesis, and Biological Evaluation of Sphingolipid-Derived Sphingosine-1 Phosphate Receptor 1 Agonists
… to be potentially arduous, well established peptide coupling techniques have been used to generate a larger amount of amide–linked analogs in a relatively short amount of time. These obtained “meta drugs” feature very similar bioactive characteristics as their all–carbon counterparts yet are …