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Titolo:
New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with alpha(2)-adrenoceptor antagonist activity
Autore:
Mayer, P; Brunel, P; Chaplain, C; Piedecoq, C; Calmel, F; Schambel, P; Chopin, P; Wurch, T; Pauwels, PJ; Marien, M; Vidaluc, JL; Imbert, T;
Indirizzi:
Ctr Rech Pierre Fabre, Div Med Chem, F-81100 Castres, France Ctr Rech Pierre Fabre Castres France F-81100 em, F-81100 Castres, France Ctr Rech Pierre Fabre, Dept Analyt Chem, F-81100 Castres, France Ctr Rech Pierre Fabre Castres France F-81100 em, F-81100 Castres, France Ctr Rech Pierre Fabre, Div Neurobiol, F-81100 Castres, France Ctr Rech Pierre Fabre Castres France F-81100 ol, F-81100 Castres, France Ctr Rech Pierre Fabre, Dept Cellular & Mol Biol, F-81100 Castres, France Ctr Rech Pierre Fabre Castres France F-81100 ol, F-81100 Castres, France
Titolo Testata:
JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 20, volume: 43, anno: 2000,
pagine: 3653 - 3664
SICI:
0022-2623(20001005)43:20<3653:NS1D>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
ALPHA-ADRENORECEPTOR REAGENTS; ALPHA-2-ADRENORECEPTOR ANTAGONISTS; PARKINSONS-DISEASE; RING-SYSTEM; YOHIMBINE; RECEPTORS; SIGNS; MPTP;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Vidaluc, JL Ctr Rech Pierre Fabre, Div Med Chem, 17 Ave Jean Moulin, F-81100 Castres, France Ctr Rech Pierre Fabre 17 Ave Jean Moulin Castres FranceF-81100
Citazione:
P. Mayer et al., "New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with alpha(2)-adrenoceptor antagonist activity", J MED CHEM, 43(20), 2000, pp. 3653-3664

Abstract

The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at alpha(2)-adrenoceptors. A series of substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl) piperidin-4-yl derivatives bearing an amide, urea, or imidazolidinone moiety was studied. Some members of this series of compounds proved to be potent alpha(2)-adrenoceptor antagonists with good selectivity versus alpha(1)-adrenergic and D-2-dopaminereceptors. Particular emphasis is given to compound 33g which displays potent alpha(2)-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 07:36:46