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Titolo:
Effects of two-carbon bridge region methoxylation of benztropine: Discovery of novel chiral ligands for the dopamine transporter
Autore:
Simoni, D; Roberti, M; Rondanin, R; Baruchello, R; Rossi, M; Invidiata, FP; Merighi, S; Varani, K; Gessi, S; Borea, PA; Marino, S; Cavallini, S; Bianchi, C; Siniscalchi, A;
Indirizzi:
Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy Univ Ferrara Ferrara Italy I-44100 Sci Farmaceut, I-44100 Ferrara, Italy Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy Univ Bologna Bologna Italy I-40126 Sci Farmaceut, I-40126 Bologna, Italy Univ Palermo, Dipartimento Farmacochim Tossicol & Biol, I-90133 Palermo, Italy Univ Palermo Palermo Italy I-90133 ssicol & Biol, I-90133 Palermo, Italy Univ Ferrara, Dipartimento Med Clin & Sperimentale, Sez Farmacol, I-44100 Ferrara, Italy Univ Ferrara Ferrara Italy I-44100 Sez Farmacol, I-44100 Ferrara, Italy
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 6, volume: 11, anno: 2001,
pagine: 823 - 827
SICI:
0960-894X(20010326)11:6<823:EOTBRM>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
SUBSTITUTED 3-ALPHA-TROPANE ANALOGS; NON-NITROGEN INHIBITORS; ENANTIOSELECTIVE SYNTHESIS; 7-METHOXYLATED COCAINE; MONOAMINE TRANSPORTERS; ABSOLUTE-CONFIGURATION; ATTRIBUTION; BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
19
Recensione:
Indirizzi per estratti:
Indirizzo: Simoni, D Univ Ferrara, Dipartimento Sci Farmaceut, Via Fossato di Mortara17-19, I-44100 Ferrara, Italy Univ Ferrara Via Fossato di Mortara 17-19 Ferrara Italy I-44100
Citazione:
D. Simoni et al., "Effects of two-carbon bridge region methoxylation of benztropine: Discovery of novel chiral ligands for the dopamine transporter", BIOORG MED, 11(6), 2001, pp. 823-827

Abstract

6-Methoxylated and 8-oxygenated benztropines were prepared and evaluated for their DAT and SERT activity (binding and uptake inhibition). Methoxylation at the two-carbon bridge of benztropine produced a novel class of potentand selective DAT ligands. An interesting enantioselectivity was also observed for this new class of chiral benztropines. The inactivity of the 8-oxygenated analogues seems to point out that, unlike cocaine and its analogues, interactions of benztropine ligands with DAT may be strongly governed by the nitrogen atom. (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 08:38:36