Title |
In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models
|
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Published in |
Drug Design, Development and Therapy, November 2013
|
DOI | 10.2147/dddt.s51298 |
Pubmed ID | |
Authors |
Sarah Schleiferböck, Christian Scheurer, Masataka Ihara, Isamu Itoh, Ian Bathurst, Jeremy N Burrows, Pascal Fantauzzi, Julie Lotharius, Susan A Charman, Julia Morizzi, David M Shackleford, Karen L White, Reto Brun, Sergio Wittlin |
Abstract |
The objective of this work was to characterize the in vitro (Plasmodium falciparum) and in vivo (Plasmodium berghei) activity profile of the recently discovered lead compound SSJ-183. The molecule showed in vitro a fast and strong inhibitory effect on growth of all P. falciparum blood stages, with a tendency to a more pronounced stage-specific action on ring forms at low concentrations. Furthermore, the compound appeared to be equally efficacious on drug-resistant and drug-sensitive parasite strains. In vivo, SSJ-183 showed a rapid onset of action, comparable to that seen for the antimalarial drug artesunate. SSJ-183 exhibited a half-life of about 10 hours and no significant differences in absorption or exposure between noninfected and infected mice. SSJ-183 appears to be a promising new lead compound with an attractive antimalarial profile. |
X Demographics
Geographical breakdown
Country | Count | As % |
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Switzerland | 1 | 50% |
Unknown | 1 | 50% |
Demographic breakdown
Type | Count | As % |
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Practitioners (doctors, other healthcare professionals) | 2 | 100% |
Mendeley readers
Geographical breakdown
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United States | 1 | 3% |
Portugal | 1 | 3% |
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Unknown | 26 | 87% |
Demographic breakdown
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Researcher | 4 | 13% |
Other | 3 | 10% |
Student > Bachelor | 2 | 7% |
Student > Postgraduate | 2 | 7% |
Other | 6 | 20% |
Unknown | 8 | 27% |
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Chemistry | 6 | 20% |
Medicine and Dentistry | 3 | 10% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 7% |
Computer Science | 1 | 3% |
Other | 3 | 10% |
Unknown | 9 | 30% |