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https://cris.library.msu.ac.zw//handle/11408/4922
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DC Field | Value | Language |
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dc.contributor.author | Tukulula, Matshawandile | - |
dc.contributor.author | Njoroge, Mathew | - |
dc.contributor.author | Abay, Efrem T. | - |
dc.contributor.author | Mugumbate, Grace C. | - |
dc.contributor.author | Wiesner, Lubbe | - |
dc.contributor.author | Taylor, Dale | - |
dc.contributor.author | Gibhard, Liezl | - |
dc.contributor.author | Norman, Jennifer | - |
dc.contributor.author | Swart, Kenneth J. | - |
dc.contributor.author | Gut, Jiri | - |
dc.contributor.author | Rosenthal, Philip J. | - |
dc.contributor.author | Barteau, Samuel | - |
dc.contributor.author | Streckfuss, Judith | - |
dc.contributor.author | Kameni-Tcheudji, Jacques | - |
dc.contributor.author | Chibale, Kelly | - |
dc.date.accessioned | 2022-06-28T12:30:04Z | - |
dc.date.available | 2022-06-28T12:30:04Z | - |
dc.date.issued | 2013 | - |
dc.identifier.issn | 1948-5875 | - |
dc.identifier.uri | https://doi.org/10.1021/ml400311r | - |
dc.identifier.uri | http://hdl.handle.net/11408/4922 | - |
dc.description.abstract | A new class of 4-aminoquinolines was synthesized and evaluated in vitro for antiplasmodial activity against both the chloroquine-sensitive (3D7) and -resistant (K1 and W2) strains. The most active compounds 3c–3e had acceptable cytotoxicity but showed strong inhibition toward a panel of cytochrome P450 enzymes in vitro. Pharmacokinetic studies on 3d and 3e in mice showed that they had moderate half-life (4–6 h) and low oral bioavailability. The front runner compound 3d exhibited moderate inhibition of the malaria parasite on P. berghei infected mice following oral administration (5 mg/kg), achieving reduction of parasitemia population by 47% on day 7. | en_US |
dc.language.iso | en | en_US |
dc.publisher | American Chemical Society | en_US |
dc.relation.ispartofseries | ACS Medicinal Chemistry Letters;Volume 4, No. 12; pages 1198-1202 | - |
dc.subject | Aminoquinolines | en_US |
dc.subject | antiplasmodial activity | en_US |
dc.subject | pharmacokinetics | en_US |
dc.subject | Plasma protein binding | en_US |
dc.title | Synthesis and in Vitro and in Vivo Pharmacological Evaluation of New 4-Aminoquinoline-Based Compounds | en_US |
dc.type | Article | en_US |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.cerifentitytype | Publications | - |
item.openairetype | Article | - |
item.fulltext | With Fulltext | - |
item.grantfulltext | open | - |
item.languageiso639-1 | en | - |
Appears in Collections: | Research Papers |
Files in This Item:
File | Description | Size | Format | |
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Synthesis and in Vitro.pdf | Abstract | 80.88 kB | Adobe PDF | View/Open |
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