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Journal article

Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.

Abstract:

New antimalarials are urgently needed. We have shown that tetrahydroquinoline (THQ) protein farnesyltransferase (PFT) inhibitors (PFTIs) are effective against the Plasmodium falciparum PFT and are effective at killing P. falciparum in vitro. Previously described THQ PFTIs had limitations of poor oral bioavailability and rapid clearance from the circulation of rodents. In this paper, we validate both the Caco-2 cell permeability model for predicting THQ intestinal absorption and the in vitro l...

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Publication status:
Published

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Publisher copy:
10.1128/aac.00246-07

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Journal:
Antimicrobial agents and chemotherapy
Volume:
51
Issue:
10
Pages:
3659-3671
Publication date:
2007-10-05
DOI:
EISSN:
1098-6596
ISSN:
0066-4804
URN:
uuid:bd8d926e-df04-4517-842e-2b608f54a244
Source identifiers:
117676
Local pid:
pubs:117676

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