- 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...
Expand abstract - Publication status:
- Published
- 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
- Language:
- English
- Keywords:
- Copyright date:
- 2007
Journal article
Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.
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