Antimalarial benzo[c]phenanthridines

James M. Nyangulu; Samantha L. Hargreaves; Susan L. Sharples; Simon P. Mackay; Roger D. Waigh; Olivier Duval; Eddie K. Mberu; William M. Watkins

doi:10.1016/j.bmcl.2005.02.074

Antimalarial benzo[c]phenanthridines

James M. Nyangulu, Samantha L. Hargreaves, Susan L. Sharples, Simon P. Mackay, Roger D. Waigh^*, Olivier Duval, Eddie K. Mberu, William M. Watkins

^*Corresponding author for this work

Strathclyde Institute Of Pharmacy And Biomedical Sciences

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

45 Citations (Scopus)

Abstract

Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC₅₀ below 5 ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC₅₀ below 30 ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.

Original language	English
Pages (from-to)	2007-2010
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2005.02.074
Publication status	Published - 15 Apr 2005

Keywords

antimalarial
hloroquine-sensitive strain
hloroquine-resistant strain

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10.1016/j.bmcl.2005.02.074

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title = "Antimalarial benzo[c]phenanthridines",

abstract = "Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC50 below 5 ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC50 below 30 ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.",

keywords = "antimalarial, hloroquine-sensitive strain, hloroquine-resistant strain",

author = "Nyangulu, \{James M.\} and Hargreaves, \{Samantha L.\} and Sharples, \{Susan L.\} and Mackay, \{Simon P.\} and Waigh, \{Roger D.\} and Olivier Duval and Mberu, \{Eddie K.\} and Watkins, \{William M.\}",

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doi = "10.1016/j.bmcl.2005.02.074",

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T1 - Antimalarial benzo[c]phenanthridines

AU - Nyangulu, James M.

AU - Hargreaves, Samantha L.

AU - Sharples, Susan L.

AU - Mackay, Simon P.

AU - Waigh, Roger D.

AU - Duval, Olivier

AU - Mberu, Eddie K.

AU - Watkins, William M.

PY - 2005/4/15

Y1 - 2005/4/15

N2 - Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC50 below 5 ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC50 below 30 ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.

AB - Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC50 below 5 ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC50 below 30 ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.

KW - antimalarial

KW - hloroquine-sensitive strain

KW - hloroquine-resistant strain

UR - https://www.scopus.com/pages/publications/15944396532

UR - https://www.sciencedirect.com/journal/bioorganic-and-medicinal-chemistry-letters

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DO - 10.1016/j.bmcl.2005.02.074

M3 - Article

C2 - 15808457

AN - SCOPUS:15944396532

SN - 0960-894X

VL - 15

SP - 2007

EP - 2010

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Antimalarial benzo[c]phenanthridines

Abstract

Keywords

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