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

doi:10.1021/jm800106u

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

Biochemistry & Molecular Biology

Research output: Contribution to journal › Article › peer-review

59 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	1995-1998
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	7
DOIs	https://doi.org/10.1021/jm800106u
State	Published - Apr 10 2008

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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10.1021/jm800106u

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title = "Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines",

abstract = "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.",

author = "Kimberly Yearick and Kekeli Ekoue-Kovi and Iwaniuk, {Daniel P.} and Natarajan, {Jayakumar K.} and John Alumasa and {De Dios}, {Angel C.} and Roepe, {Paul D.} and Christian Wolf",

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AU - Yearick, Kimberly

AU - Ekoue-Kovi, Kekeli

AU - Iwaniuk, Daniel P.

AU - Natarajan, Jayakumar K.

AU - Alumasa, John

AU - De Dios, Angel C.

AU - Roepe, Paul D.

AU - Wolf, Christian

PY - 2008/4/10

Y1 - 2008/4/10

N2 - 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.

AB - 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.

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JF - Journal of Medicinal Chemistry

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ER -

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

Abstract

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