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Titolo:
SYNTHESIS AND EVALUATION OF 6,11-ETHANOHEXAHYDROBENZO[B]QUINOLIZIDINES - A NEW CLASS OF NONCOMPETITIVE N-METHYL-D-ASPARTATE ANTAGONISTS
Autore:
SUBRAMANYAM C; MALLAMO JP; PILLING GM; EARLEY WG; CARABATEAS PM; WETZEL JR; DEHAVENHUDKINS D; ALLEN T; KULLNIG RK;
Indirizzi:
CEPHALON INC,145 BRANDYWINE PKWY W CHESTER PA 19380 SANOFI WINTHROP INC,DIV RES,DEPT MED CHEM COLLEGEVILLE PA 19426 SANOFI WINTHROP INC,DIV RES,DEPT BIOCHEM COLLEGEVILLE PA 19426 SANOFI WINTHROP INC,DIV RES,DEPT MOLEC CHARACTERIZ COLLEGEVILLE PA 19426
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 13, volume: 38, anno: 1995,
pagine: 2483 - 2489
SICI:
0022-2623(1995)38:13<2483:SAEO6>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
CENTRAL NERVOUS-SYSTEM; PHENCYCLIDINE-LIKE; ACID; PHARMACOLOGY; MK-801; DRUGS; DISORDERS; RECEPTORS; MODEL;
Tipo documento:
Note
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
C. Subramanyam et al., "SYNTHESIS AND EVALUATION OF 6,11-ETHANOHEXAHYDROBENZO[B]QUINOLIZIDINES - A NEW CLASS OF NONCOMPETITIVE N-METHYL-D-ASPARTATE ANTAGONISTS", Journal of medicinal chemistry, 38(13), 1995, pp. 2483-2489

Abstract

The synthesis and in vitro and in vivo evaluation of 2,13-cycloalkyl-6,11-ethanobenzo[b]quinolizidines, a new class of noncompetitive N-methyl-D-aspartate (NMDA) antagonists acting at the PCP site on the NMDA receptor complex, is reported. Structure-activity relationship studiesled to the identification of 10-hydroxy-(6 alpha,11 alpha,11 alpha ',2']-endo-cyclopenta-2H-pyrido[1,2-b]isoquinoline hydrobromide (5h) and9-hydroxy-(6 alpha,11 alpha,11 alpha ',2']-endo-cyclopenta-2H-pyrido[1,2-b]isoquinoline hydrobromide(5i), the most potent members of this series with K-i values of 2.3 +/- 0.2 and 2.3 +/- 0.5 nM, respectively. Molecular modeling studies revealed that this series of compounds occupies both lipophilic sites of the Andrews PCP receptor model and shares structural features which are common to other classes of known noncompetitive NMDA antagonists such as MK-801.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/11/20 alle ore 03:30:09