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Showing 1 to 6 of 6 for “"lactamisation"”.
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Aspects of the mechanisms of alkaline hydrolysis of amino acid esters
… linear. For some esters, the E form undergoes lactamisation with a large rate constant, kL, which replaces the negligibly small kE. The kE values for the methyl, ethyl and benzyl esters of 2-AE, 3-AP, 6-AH and 4-DMAB, and the kE8+ values for all of the esters, are consistent with a simple BAc2 …
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Synthesis of multicyclic ring systems including an alternate route to Meyers’ lactam derivatives
… lactams by utilising the use of Meyers’ lactamisation methodology. This provided high atroposelection through a central C5 to axial chirality transfer. The aim of this project will be directed towards the design of alternative strategies in the synthesis of keto-ester Meyers’ lactam …
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The synthesis and metal ion catalysed hydrolysis of methyl 4,5-diaminopentanoate
… rapid, pair of intramolecular aminolysis (lactamisation) reactions. These involve competition between five and six membered lactam ring closure. Overall constants of the order 10³ℓmol⁻¹s⁻¹ at 25°C and I = 0.10molℓ⁻¹ are observed. The Cu(II) catalysed hydrolysis of methyl …
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Towards Inhibition of Oncogenic RhoA Signaling using Stapled Peptides
… an IC50 of 2.1 mM. All-hydrocarbon stapling and lactamisation of the peptide at the N-terminal 50-54 residues increased α-helicity to around 50%, but did not improve RhoA binding affinity. A series of mutations on the linear peptide were screened to identify those with improved binding affinity, …
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Chlorinated amino acids in peptide production
A new method for the production of peptides through biological expression was developed, utilising lactonisation-prone chlorinated amino acids for latent peptide bond digestion. Incorporation of halogenated amino acids into proteins is possible due to the inherent inability of the biological …
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Chlorinated amino acids in peptide production
A new method for the production of peptides through biological expression was developed, utilising lactonisation-prone chlorinated amino acids for latent peptide bond digestion. Incorporation of halogenated amino acids into proteins is possible due to the inherent inability of the biological …