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Titolo:
2-arylpyrazolo[1,5-a]pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands
Autore:
Selleri, S; Bruni, F; Costagli, C; Costanzo, A; Guerrini, G; Ciciani, G; Costa, B; Martini, C;
Indirizzi:
Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy Univ Florence Florence Italy I-50121 Farmaceut, I-50121 Florence, Italy Univ Pisa, Dipartimento Psichiat Neurobiol Farmacol & Biotec, I-56126 Pisa, Italy Univ Pisa Pisa Italy I-56126 biol Farmacol & Biotec, I-56126 Pisa, Italy
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 10, volume: 9, anno: 2001,
pagine: 2661 - 2671
SICI:
0968-0896(200110)9:10<2661:2ANPAS>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
BINDING-SITES; RAT-BRAIN; 2-PHENYLIMIDAZO<1,2-A>PYRIDINE DERIVATIVES; HIGH-AFFINITY; MITOCHONDRIA; MEMBRANES; DIAZEPAM; 1-(2-CHLOROPHENYL)-N-METHYL-N-(1-METHYLPROPYL)-3-ISOQUINOLINECARBOXAMIDE; IMIDAZOPYRIDINES; LOCALIZATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
59
Recensione:
Indirizzi per estratti:
Indirizzo: Bruni, F Univ Florence, Dipartimento Sci Farmaceut, Via G Capponi 9, I-50121 Florence, Italy Univ Florence Via G Capponi 9 Florence Italy I-50121 ence, Italy
Citazione:
S. Selleri et al., "2-arylpyrazolo[1,5-a]pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands", BIO MED CH, 9(10), 2001, pp. 2661-2671

Abstract

A new class of N,N-diethyl-(2-arylpyrazolo[1,5-a]pyrimidin-3-yl)acetamides(3f-y), as azaisosters of Alpidem, was prepared following a novel synthetic method and their affinities for both the peripheral (PBR) and the central(CBR) benzodiazepine receptors were evaluated. Binding assays were carriedout using both [H-3]PK 11195 and [H-3]Ro 5-4864 as radioligands for PBR, whereas [H-3]Ro 15-1788 was used for CBR, in rat kidney and rat cortex, respectively. The tested compounds exhibited a broad range of binding affinities from as low as 0.76 nM to inactivity and most of them proved to be high selective ligands for PBR. The preliminary SAR studies suggested some of thestructural features required for high affinity and selectivity; particularly the substituents on the pyrimidine moiety seemed to play an important role in PBR versus CBR selectivity. A subset of the highest affinity compounds was also tested for their ability to stimulate steroid biosynthesis in C6glioma rat cells and some of these were found to increase pregnenolone formation with potency similar to Ro 5-4864 and PK 11195. (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 23/01/20 alle ore 03:30:43