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Titolo:
Dynamic deconvolution of a pre-equilibrated dynamic combinatorial library of acetylcholinesterase inhibitors
Autore:
Bunyapaiboonsri, T; Ramstrom, O; Lohmann, S; Lehn, JM; Peng, L; Goeldner, M;
Indirizzi:
Univ Strasbourg 1, ISIS, Lab Chim Supramol, CNRS,UPRES A 7006, F-67000 Strasbourg, France Univ Strasbourg 1 Strasbourg France F-67000 , F-67000 Strasbourg, France Univ Louis Pasteur Strasbourg 1, Fac Pharm, Chim Bioorgan Lab, CNRS,UMR 7514, F-67401 Illkirch Graffenstaden, France Univ Louis Pasteur Strasbourg 1Illkirch Graffenstaden France F-67401 ce
Titolo Testata:
CHEMBIOCHEM
fascicolo: 6, volume: 2, anno: 2001,
pagine: 438 - 444
SICI:
1439-4227(20010601)2:6<438:DDOAPD>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
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;
Keywords:
acetylcholinesterase; combinatorial chemistry; enzyme catalysis; hydrolases; inhibitors;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
83
Recensione:
Indirizzi per estratti:
Indirizzo: Lehn, JM Univ Strasbourg 1, ISIS, Lab Chim Supramol, CNRS,UPRES A 7006, 4 Rue Blaise Pascal, F-67000 Strasbourg, France Univ Strasbourg 1 4 Rue Blaise Pascal Strasbourg France F-67000
Citazione:
T. Bunyapaiboonsri et al., "Dynamic deconvolution of a pre-equilibrated dynamic combinatorial library of acetylcholinesterase inhibitors", CHEMBIOCHEM, 2(6), 2001, pp. 438-444

Abstract

A dynamic combinatorial library composed of interconverting acylhydrazoneshas been generated and screened towards inhibition of acetylcholinesterasefrom the electric ray Torpedo marmorata. Starting from a small set (13) ofinitial 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.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 12:35:01