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Titolo:
"One-pot" synthesis and antimalarial activity of formamidine derivatives of 4-anilinoquinoline
Autore:
Delarue, S; Girault, S; Ali, FD; Maes, L; Grellier, P; Sergheraert, C;
Indirizzi:
Univ Lille 2, Fac Pharm, Inst Biol, CNRS,UMR 8525, F-59021 Lille, France Univ Lille 2 Lille France F-59021 , CNRS,UMR 8525, F-59021 Lille, France Univ Lille 2, Fac Pharm, Inst Pasteur, F-59021 Lille, France Univ Lille 2Lille France F-59021 m, Inst Pasteur, F-59021 Lille, France Museum Natl Hist Nat, Lab Biol Parasitaire, CNRS, IFR 63, F-75005 Paris, France Museum Natl Hist Nat Paris France F-75005 IFR 63, F-75005 Paris, France TIBOTEC, B-32800 Mechelen, Belgium TIBOTEC Mechelen Belgium B-32800TIBOTEC, B-32800 Mechelen, Belgium
Titolo Testata:
CHEMICAL & PHARMACEUTICAL BULLETIN
fascicolo: 8, volume: 49, anno: 2001,
pagine: 933 - 937
SICI:
0009-2363(200108)49:8<933:"SAAAO>2.0.ZU;2-J
Fonte:
ISI
Lingua:
ENG
Soggetto:
AMODIAQUINE-INDUCED AGRANULOCYTOSIS; MECHANISMS; RAT;
Keywords:
drug design; malaria; Plasmodium falciparum; chloroquine; amodiaquine; formamidine;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
19
Recensione:
Indirizzi per estratti:
Indirizzo: Sergheraert, C Univ Lille 2, Fac Pharm, Inst Biol, CNRS,UMR 8525, 1 Rue Prof Calmette,BP 447, F-59021 Lille, France Univ Lille 2 1 Rue Prof Calmette,BP 447 Lille France F-59021
Citazione:
S. Delarue et al., ""One-pot" synthesis and antimalarial activity of formamidine derivatives of 4-anilinoquinoline", CHEM PHARM, 49(8), 2001, pp. 933-937

Abstract

Amodiaquine (AQ) is an antimalarial which is effective against chloroquino-resistant strains of Plasmodium falciparum but whose clinical use is severely restricted because of associated hepatotoxicity and agranulocytosis. "One-pot" synthesis of formamidines likely to be transformed into AQ derivatives is reported. Compared with AQ, the new compounds were devoid of in vitro cytotoxicity upon human embryonic lung cells and mouse peritoneal macrophages. One showed a potent in vivo activity in mice infected with P. berghei. Transformation of this compound by reductive amination led to a new type of AQ derivatives that displayed an in vitro activity similar to that of AQbut did not lead to toxic quinone-imines.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 10:31:08