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Dynamic deconvolution of a pre-equilibrated dynamic combinatorial library of acetylcholinesterase inhibitors
KTH, Superseded Departments, Chemistry.
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2001 (English)In: ChemBioChem (Print), ISSN 1439-4227, E-ISSN 1439-7633, Vol. 2, no 6, 438-444 p.Article in journal (Refereed) Published
Abstract [en]

A dynamic combinatorial library composed of interconverting acylhydrazones has been generated and screened towards inhibition of acetylcholinesterase from the electric ray Torpedo marmorata. Starting from a small set (13) of initial hydrazide and aldehyde building blocks, a library containing possibly 66 different species was obtained in a single operation. Of all possible acylhydrazones formed, active compounds containing two terminal cationic recognition groups separated by an appropriate distance, permitting two-site binding, could be rapidly identified by using a dynamic deconvolution-screening procedure, based on the sequential removal of starting building blocks. A very potent bis-pyridinium inhibitor (K (i)= 1.09 nM, alphaK(i) = 2.80 nM) was selected from the process and the contribution of various structural features to inhibitory potency was evaluated.

Place, publisher, year, edition, pages
2001. Vol. 2, no 6, 438-444 p.
Keyword [en]
acetylcholinesterase, combinatorial chemistry, enzyme catalysis, hydrolases, inhibitors, hydrogen-bonded assemblies, drive chemical evolution, dna-binding compounds, alzheimers-disease, molecular recognition, pd(ii)-linked cages, directed synthesis, self-recognition, ligand-binding, drug discovery
URN: urn:nbn:se:kth:diva-20697ISI: 000169168600007OAI: diva2:339393
QC 20100525Available from: 2010-08-10 Created: 2010-08-10Bibliographically approved

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