51848-56-7Relevant articles and documents
Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies
Ammazzalorso, Alessandra,Carradori, Simone,Angeli, Andrea,Akdemir, Atilla,De Filippis, Barbara,Fantacuzzi, Marialuigia,Giampietro, Letizia,Maccallini, Cristina,Amoroso, Rosa,Supuran, Claudiu T.
, p. 1051 - 1061 (2019)
A large library of fibrate-based N-acylsulphonamides was designed, synthesised, and fully characterised in order to propose them as zinc binders for the inhibition of human carbonic anhydrase (hCA) enzymatic activity. Synthesised compounds were tested aga
METHODS OF IDENTIFYING CROSSLINKING MOLECULES FOR POLYMERS
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Paragraph 0112; 0113, (2015/06/03)
Methods for screening molecules or moieties for their ability to crosslink are disclosed. An aromatic carbonate, aromatic ester, or aliphatic ester group is attached to the molecule to mimic the presence of a polymer. A solution of the modified molecule i
Benzhydrylamine linker grafting: A strategy for the improved synthesis of C-terminal peptide amides
Alewood, Dianne,Hopping, Gene,Brust, Andreas,Reid, Robert C.,Alewood, Paul F.
experimental part, p. 551 - 557 (2011/11/12)
The standard p-MBHA resin used during Boc-chemistry synthesis of peptides carrying C-terminal carboxamides is compromised by batch-to-batch variations in its performance. This can cause artificially 'difficult' couplings during peptide chain assembly, which may ultimately lead to failed syntheses given the inability to achieve acceptable coupling yields. To overcome these problems, we have developed a new approach by grafting a functionalized benzhydrylamine linker onto well-characterized and well-performing PAM resins. We combine optimized Boc-chemistry, high-performing PAM resins and new benzhydrylamine-based linkers to achieve improved syntheses of peptide amides. Here we present the synthesis of two new benzhydrylamine linkers and their attachment to selected PAM resins. This novel solid support was evaluated through the synthesis of selected 'difficult' conotoxins and monitoring the coupling efficiency using quantitative ninhydrin assay. The results show a superior performance of the novel linker solid support compared to the standard p-MBHA resins routinely used. In summary, we describe an alternative linker-resin system that allows improved access to C-terminal amide peptides employing Boc/Bzl chemistry. Benzhydrylamine enzhydrylamine linkers (a/b) were grafted onto high-performing Phe-PAM resins for Boc solid phase peptide amide synthesis. Fast couplings with high fidelity were achieved enabling the synthesis of selected conotoxins that previously demonstrated artificially 'difficult sequences' on commercially available p-MBHA resins. Copyright
