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Titolo:
New 4-aminoquinoline mannich base antimalarials. 1. Effect of an alkyl substituent in the 5 '-position of the 4 '-hydroxyanilino side chain
Autore:
Raynes, KJ; Stocks, PA; ONeill, PM; Park, BK; Ward, SA;
Indirizzi:
Univ Liverpool, Dept Pharmacol & Therapeut, Liverpool L69 3GE, Merseyside,England Univ Liverpool Liverpool Merseyside England L69 3GE E, Merseyside,England Univ Liverpool, Dept Chem, Liverpool L69 3GE, Merseyside, England Univ Liverpool Liverpool Merseyside England L69 3GE , Merseyside, England
Titolo Testata:
JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 15, volume: 42, anno: 1999,
pagine: 2747 - 2751
SICI:
0022-2623(19990729)42:15<2747:N4MBA1>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
AMODIAQUINE-INDUCED AGRANULOCYTOSIS; PLASMODIUM-FALCIPARUM; PHYSICOCHEMICAL PROPERTIES; FERRIPROTOPORPHYRIN-IX; UNCOMPLICATED MALARIA; CHLOROQUINE; RESISTANCE; IDENTIFICATION; CHILDREN; INVITRO;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
32
Recensione:
Indirizzi per estratti:
Indirizzo: Ward, SA Univ Liverpool, Dept Pharmacol & Therapeut, POB 147, Liverpool L69 3GE, Merseyside, England Univ Liverpool POB 147 Liverpool Merseyside England L69 3GE gland
Citazione:
K.J. Raynes et al., "New 4-aminoquinoline mannich base antimalarials. 1. Effect of an alkyl substituent in the 5 '-position of the 4 '-hydroxyanilino side chain", J MED CHEM, 42(15), 1999, pp. 2747-2751

Abstract

A new series of 4-aminoquinoline Mannich base derivatives have been synthesized, in which the 3'-diethylamino function of amodiaquine (AQ) is replaced by a 3'-tert-butylamino group and an aliphatic hydrocarbon entity is incorporated into the 5'-position of the 4'-hydroxyanilino side chain. Seven alkyl Mannich base derivatives were screened and found to be active against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. The propyl and isopropyl alkyl derivatives were found to be! the most active; consequently these derivatives were tested against a nonsensitive strain of Plasmodium, berghi in vivo and found to be 3-fold more active than AQ, irrespective of the route of administration (oral or intraperitoneal).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 00:59:09