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Titolo:
SYNTHESIS AND BENZODIAZEPINE RECEPTOR-BINDING OF SOME IMIDAZO[2,1-B]BENZOXAZOLE, PYRIMIDO[2,1-B]BENZOXAZOLE AND PYRIMIDO[1,2-A]BENZIMIDAZOLES
Autore:
TRAPANI G; FRANCO M; LATROFA A; GENCHI G; IACOBAZZI V; GHIANI CA; MACIOCCO E; LISO G;
Indirizzi:
UNIV BARI,FAC FARM,DIPARTIMENTO FARMACOCHIM,VIA ORABONA 4 I-70125 BARI ITALY UNIV BARI,FAC FARM,DIPARTIMENTO BIOL SPERIMENTALE I-70125 BARI ITALY
Titolo Testata:
European journal of medicinal chemistry
fascicolo: 1, volume: 32, anno: 1997,
pagine: 83 - 89
SICI:
0223-5234(1997)32:1<83:SABROS>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Keywords:
IMIDAZO[2,1-B]BENZOXAZOLE; PYRIMIDO[2,1-B]BENZOXAZOLE; PYRIMIDO[1,2-A]BENZIMIDAZOLE; CENTRAL BENZODIAZEPINE RECEPTOR; PERIPHERAL BENZODIAZEPINE RECEPTOR; [S-35] TBPS BINDING; GABA RATIO;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
11
Recensione:
Indirizzi per estratti:
Citazione:
G. Trapani et al., "SYNTHESIS AND BENZODIAZEPINE RECEPTOR-BINDING OF SOME IMIDAZO[2,1-B]BENZOXAZOLE, PYRIMIDO[2,1-B]BENZOXAZOLE AND PYRIMIDO[1,2-A]BENZIMIDAZOLES", European journal of medicinal chemistry, 32(1), 1997, pp. 83-89

Abstract

A series of imidazo[2,1-b]benzoxazoles 3a-c, pyrimido[2,1-b]benzoxazoles 4-6, and pyrimido[1,2-a]benzimidazoles 7-9 was synthesized and evaluated for affinity at the benzodiazepine receptor (BZR). These compounds generally possess BZR binding affinities lower than those observedfor the corresponding benzothiazole analogues. However, imidazobenzoxazole 3d possesses high binding affinity, showing an IC50 value of 77 nM. The pharmacological profile of 3d was predicted by [S-35]TBPS binding as inverse agonist whereas antagonist or partial agonist activity was suggested by the GABA ratio value. Hence, a contrasting predictivecapability of GABA ratio and [S-35]TBPS binding was observed. Compound 3d should possess partial inverse agonist activity at BZR, because its [S-35]TBPS binding data is comparable to those of FG-7142.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/06/20 alle ore 02:22:44