Journal of Medicinal Chemistry 2008-04-10

Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines.

Kimberly Yearick, Kekeli Ekoue-Kovi, Daniel P Iwaniuk, Jayakumar K Natarajan, John Alumasa, Angel C de Dios, Paul D Roepe, Christian Wolf

文献索引：J. Med. Chem. 51(7) , 1995-8, (2008)

全文：HTML全文

摘要

Systematic variation of the branching and basicity of the side chain of chloroquine yielded a series of new 7-chloro-4-aminoquinoline derivatives exhibiting high in vitro activity against four different strains of P. falciparum. Many of the compounds tested showed excellent potency against chloroquine sensitive and resistant strains. In particular 4b, 5a, 5b, 5d, 17a, and 17b were found to be significantly more potent than chloroquine against the resistant strains Dd2 and FCB.

相关化合物

  • 4-氨基-7-氯喹啉

相关文献：

New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton.

2008-10-09

[J. Med. Chem. 51(19) , 6216-9, (2008)]

An ELISA test for detecting chloroquine in urine.

1988-01-01

[Trans. R. Soc. Trop. Med. Hyg. 82(2) , 216-20, (1988)]

Synthesis and comparison of antiplasmodial activity of (+), (-) and racemic 7-chloro-4-(N-lupinyl)aminoquinoline.

2012-10-01

[Bioorg. Med. Chem. 20(19) , 5980-5, (2012)]

Chloroquine metabolism in man: urinary excretion of 7-chloro-4-hydroxyquinoline and 7-chloro-4-aminoquinoline metabolites.

[J. Chromatogr. A. 345(1) , 209-14, (1985)]

Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines.

2010-09-15

[Bioorg. Med. Chem. 18(18) , 6625-33, (2010)]

更多文献...