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Titolo:
SAR studies of piperidine-based analogues of cocaine. Part 3: Oxadiazoles
Autore:
Petukhov, PA; Zhang, M; Johnson, KJ; Tella, SR; Kozikowski, AP;
Indirizzi:
Georgetown Univ, Dept Neurol, Drug Discovery Program, Med Ctr, Washington,DC 20007 USA Georgetown Univ Washington DC USA 20007 Med Ctr, Washington,DC 20007 USA Georgetown Univ, Dept Pharmacol, Drug Discovery Program, Med Ctr, Washington, DC 20007 USA Georgetown Univ Washington DC USA 20007 Med Ctr, Washington, DC 20007 USA Univ Texas, Med Branch, Dept Pharmacol & Toxicol, Galveston, TX 77555 USA Univ Texas Galveston TX USA 77555 acol & Toxicol, Galveston, TX 77555 USA
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 16, volume: 11, anno: 2001,
pagine: 2079 - 2083
SICI:
0960-894X(20010820)11:16<2079:SSOPAO>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEROTONIN REUPTAKE INHIBITORS; DOPAMINE; TRANSPORTERS; DESIGN; BIOISOSTERISM; SELECTIVITY; CHEMISTRY; BINDING; ABUSE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Kozikowski, AP Georgetown Univ, Dept Neurol, Drug Discovery Program, Med Ctr, 3900 Reservoir Rd NW, Washington, DC 20007 USA Georgetown Univ 3900 Reservoir Rd NW Washington DC USA 20007
Citazione:
P.A. Petukhov et al., "SAR studies of piperidine-based analogues of cocaine. Part 3: Oxadiazoles", BIOORG MED, 11(16), 2001, pp. 2079-2083

Abstract

The synthesis of novel 4 beta -aryl-1-methyl-3 alpha-(3-substituted-1,2,4-oxadiazol-5-yl)piperidines, bioisosteres of ester (+)-1, is described. The synthesized oxadiazoles were evaluated for their affinity to the DAT and their ability to inhibit monoamine reuptake at the DAT. NET, and 5HTT. The results show that affinity to the DAT and ability to inhibit the reuptake at the DAT, NET, and 5HTT is a function of the size of the substituent in the oxadiazole ring. (+)-(3R,4S)-4 beta-(4-Chlorophenyl)-1-methyl-3 alpha-(3-methyl-1,2,4-oxadiazol-5-yl)piperidine [(+)-2a], which is structurally and pharmacologically most similar to the ester (+)-1 in this series, showed at least a 2-fold longer duration of action when compared to ester (+)-1. (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 19/01/20 alle ore 08:57:25