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3,3′-Disubstituted 5,5′-Bi(1,2,4-triazine) derivatives with potent in vitro and in vivo antimalarial activity

Abstract:

A series of 3,3′-disubstituted 5,5′-bi(1,2,4-triazine) derivatives was synthesized and screened against the erythrocytic stage of Plasmodium falciparum 3D7 line. The most potent dimer, 6k, with an IC50 (50% inhibitory concentration) of 0.008 μM, had high in vitro potency against P. falciparum lines resistant to chloroquine (W2, IC50 = 0.0047 ± 0.0011 μM) and artemisinin (MRA1240, IC50 = 0.0086 ± 0.0010 μM). Excellent ex vivo potency of 6k was shown against clinical field isolates of both P. f...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
62
Issue:
5
Pages:
2485–2498
Publication date:
2019-02-04
Acceptance date:
2019-02-04
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pubs id:
pubs:969838
UUID:
uuid:82a86e9f-6380-4981-9852-28db5664baa4
Source identifiers:
969838
Local pid:
pubs:969838
Language:
English

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