Tryptophan-derived butyrylcholinesterase inhibitors as promising leads against Alzheimer's disease
We have identified tryptophan-based selective nanomolar butyrylcholinesterase (BChE) inhibitors. They are defined according to their chemical modularity, novel binding mode revealed by five solved crystal structures with human BChE, low cytotoxicity, and predicted permeability of the blood-brain barrier. Altogether, these factors indicate their potential as unique lead compounds for symptomatic therapy against Alzheimer's disease.
The invention is directed to novel CCK analogs wherein Tryptophan and/or Phenylalamine are substituted with a radical which provides enhanced appetite suppressant activity to the peptide.
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(2008/06/13)
Synthesis of Unnatural Amino Acids
This communication presents efficient synthetic procedures for the D and L isomers of Nα-tert-butyloxycarbonyl-Nε-benzyloxycarbonyl-Nε-isopropyllysine dicyclohexylamine salt (Nα-Boc-Nε-Z-Ilys DCHA salt), the D and L isomers of Nα-tert-butyloxycarbonyl-Nεnicotinoyllysine (Nα-Boc-Niclys), β-(3-quinolyl)-D,L-alanine (3-Quinal), and the resolution into the D and L isomers of 3-Quinal.
Acosta, C. Kirk,Bahr, Martin L.,Burdett, James E.,Cessac, James W.,Martinez, Rudy A.,et al.
p. 914 - 934
(2007/10/02)
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