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Titolo:
ANALOGS OF THE POTENTIAL ANTIPSYCHOTIC AGENT 1192U90 - AMIDE MODIFICATIONS
Autore:
NAVAS F; TANG FLM; SCHALLER LT; NORMAN MH;
Indirizzi:
AMGEN INC,SMALL MOL DRUG DISCOVERY,1840 DE HAVILLAND DR THOUSAND OAKSCA 91320 GLAXO WELLCOME INC,DIV CHEM RES TRIANGLE PK NC 27709 GLAXO WELLCOME INC,DIV PHARMACOL & MOL THERAPEUT RES TRIANGLE PK NC 27709
Titolo Testata:
Bioorganic & medicinal chemistry
fascicolo: 6, volume: 6, anno: 1998,
pagine: 811 - 823
SICI:
0968-0896(1998)6:6<811:AOTPAA>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
CLOZAPINE-INDUCED AGRANULOCYTOSIS; D-2/5-HT2 ANTAGONISTS; DOPAMINE D-2; PHARMACOLOGY; DERIVATIVES; PROFILE; SERIES; DRUGS; SCHIZOPHRENIA; ILOPERIDONE;
Keywords:
1192U90; ANTIPSYCHOTIC; SEROTONIN 5-HT1A; SEROTONIN 5-HT2; DOPAMINE D-2;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
F. Navas et al., "ANALOGS OF THE POTENTIAL ANTIPSYCHOTIC AGENT 1192U90 - AMIDE MODIFICATIONS", Bioorganic & medicinal chemistry, 6(6), 1998, pp. 811-823

Abstract

Analogues of 2-amino-N-(4-(4-(1, 2-benzisothiazol-3 -yl)-1-piperazinyl)-butyl)benzamide hydrochloride (1192U90) were prepared and evaluatedin receptor binding assays for the dopamine D-2, serotonin 5-HT1a, and serotonin 5-HT2 receptors. Eight compounds have been synthesized in which the amide group of 1192U90 has been replaced with a variety of functional groups (i.e, ester, ketone, thioamide, butyramide, butyranilide, sulfonamide, alkoxyamide and hydrazide). These compounds exhibited moderate to potent affinities (0.55-200 nM) for all three receptors. Several analogues exhibited improved selectivity for the 5-HT2 receptor with D-2/5-HT2 binding ratios greater than 1192U90. (C) 1998 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 06:54:02