- Effect of proline analogues on the conformation of elastin peptides
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Three elastin model peptides containing the repetitive motif -VGVXGVG-, where X corresponds to (2S)-proline (Pro), (2S,4R)-4-hydroxy-proline (Hyp) and (2S,4R)-4-methoxy-proline (Mop), were synthesized in order to define the effect of the introduction of an electronegative group on the conformation and self-assembling properties of the peptides. Circular dichroism, NMR and FT-IR spectroscopies evidenced outstanding differences at molecular and supramolecular level. This work constitutes the basis for the proper design of elastin-inspired drugs with tailored conformational properties.
- Pepe, Antonietta,Crudele, Maria Antonietta,Bochicchio, Brigida
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- N-Aryl Pyrrolidine Derivatives as Beta-Secretase Inhibitors
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There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R7, and p as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
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(2010/11/28)
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