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Titolo:
Synthesis and structure-affinity relationships of 1,3,5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site
Autore:
Jirgensons, A; Kauss, V; Kalvinsh, I; Gold, MR; Danysz, W; Parsons, CG; Quack, G;
Indirizzi:
Latvian Inst Organ Synth, LV-1006 Riga, Latvia Latvian Inst Organ Synth Riga Latvia LV-1006 Synth, LV-1006 Riga, Latvia GMBH&Co, Merz & Co, D-60048 Frankfurt, Germany GMBH&Co Frankfurt GermanyD-60048 Merz & Co, D-60048 Frankfurt, Germany
Titolo Testata:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 6, volume: 35, anno: 2000,
pagine: 555 - 565
SICI:
0223-5234(200006)35:6<555:SASRO1>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
D-ASPARTATE RECEPTOR; ION CHANNEL; CYCLOHEXANONES; ANTAGONISTS; REDUCTION; ALCOHOLS; KINETICS;
Keywords:
NMDA receptor; PCP; cyclohexylamines; Hansch analysis;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Kalvinsh, I Latvian Inst Organ Synth, 21 Aizkraukles Str, LV-1006 Riga, Latvia Latvian Inst Organ Synth 21 Aizkraukles Str Riga Latvia LV-1006
Citazione:
A. Jirgensons et al., "Synthesis and structure-affinity relationships of 1,3,5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site", EUR J MED C, 35(6), 2000, pp. 555-565

Abstract

A series of 1,3,5-alkylsubstituted cyclohexylamines 2 were synthesized as ligands for the N-methyl-D-aspartate (NMDA) receptor phencyclidine (PCP) binding site. Pure diastereomers with defined configuration of amino group 2-ax and 2-eq were obtained. The optimal size of 1,3,5-substituents was determined for cyclohexylamines 2 with an equatorial amino group in the lowest energy conformation using Hansch analysis. According to the data, the lipophilic part of cyclohexylamines 2 does not discriminate between hydrophobic regions of the PCP binding site but rather recognizes this site as a whole lipophilic pocket. (C) 2000 Editions scientifiques et medicales Elsevier SAS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/03/20 alle ore 23:08:20