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Titolo:
Synthesis and biological evaluation of 2-(3 '-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist
Autore:
Costantino, G; Maltoni, K; Marinozzi, M; Camaioni, E; Prezeau, L; Pin, JP; Pellicciari, R;
Indirizzi:
Univ Perugia, Dipartimento Chim & Tecnol Farm, I-06123 Perugia, Italy UnivPerugia Perugia Italy I-06123 & Tecnol Farm, I-06123 Perugia, Italy CNRS, UPR 9023, CCIPE, F-34094 Montpellier, France CNRS Montpellier France F-34094 9023, CCIPE, F-34094 Montpellier, France
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 2, volume: 9, anno: 2001,
pagine: 221 - 227
SICI:
0968-0896(200102)9:2<221:SABEO2>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
METABOTROPIC GLUTAMATE RECEPTORS; AMINO-ACIDS; PROTEINS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
16
Recensione:
Indirizzi per estratti:
Indirizzo: Pellicciari, R Univ Perugia, Dipartimento Chim & Tecnol Farm, Via Liceo 1,I-06123 Perugia, Italy Univ Perugia Via Liceo 1 Perugia Italy I-06123 ugia, Italy
Citazione:
G. Costantino et al., "Synthesis and biological evaluation of 2-(3 '-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist", BIO MED CH, 9(2), 2001, pp. 221-227

Abstract

The design and synthesis of 2-(3'-(1H-tetrazol-5-yl)bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGluR1 antagonist is reported. S-TBPG is characterized by the bioisosteric replacement of the distal carboxy group of 2-(3'-carboxybicyclo [1.1.1]pent-1-yl)glycine (S-CBPG) by a tetrazolyl moiety. Despite a moderate reduction in potency, S-TBPG is a selective mGluR1 antagonist (69 muM), with no activity at other mCluR subtypes. The interesting biological profile of S-TBPG, coupled with its peculiar chemical structure, is discussed in terms of the structure-activity relationship (SAR) of mGluR1 antagonists. (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 02/04/20 alle ore 19:30:13