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Synthesis, characterization, and cellular localization of a fluorescent probe of the antimalarial 8-aminoquinoline primaquine.

Abstract：

:Primaquine (PQ) is the only commercially available drug that clears dormant liver stages of malaria and blocks transmission to mosquito vectors. Although an old drug, much remains to be known about the mechanism(s) of action. Herein we develop a fluorescent tagged PQ to discover cellular localization in the human malaria parasite, Plasmodium falciparum. Successful synthesis and characterization of a primaquine-coumarin fluorescent probe (PQCP) demonstrated potency equivalent to the parent drug and the probe was not cytotoxic to HepG2 carcinoma cells. Cellular localization was found primarily in the cytosol of the asexual erythrocytic and gametocyte stages of parasite development.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

McQueen A,Blake LD,Azhari A,Kemp MT,McGaha TW Jr,Namelikonda N,Larsen RW,Manetsch R,Kyle DE

doi

10.1016/j.bmcl.2017.09.030

subject

Has Abstract

pub_date

2017-10-15 00:00:00

pages

4597-4600

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)30926-5

journal_volume

27

pub_type

杂志文章

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