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33846904180
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Central Drug Research Institute CDRI
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Central Drug Research Institute (CDRI) communication number: 6920.
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communication
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0021948029
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(a) Vennerstrom, J. L., Arbe-Barens, S.; Brun, R.; Charman, S. A.; Chiu, F. C. K.; Chollet, J.; Dong, Y.; Dorn, A.; Hunziker, D.; Matile, H.; McIntosh, K.; Padmanilayam, M.; Tomas, J. S.; Scheurer, C.; Scorneaux, B.; Tang, Y.; Urwyler, H.; Urwyler, H.; Wittlin, S.; Charman, W. N. Identification of an antimalarial synthetic trioxaolane drug development candidate. Nature 2004, 430, 900.
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2-Hydroperoxy-3-(5,6,7,8-tetrahydro-naphthalen-2-yl)-but-3-en-1-ol 9c and 3-adamantan-1-yl-2-hydroperoxy-but-3-en- 1-ol 9g were not isolated and used in situ for preparation of trioxanes 13c, 13g, and 14a,b.
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2-Hydroperoxy-3-(5,6,7,8-tetrahydro-naphthalen-2-yl)-but-3-en-1-ol 9c and 3-adamantan-1-yl-2-hydroperoxy-but-3-en- 1-ol 9g were not isolated and used in situ for preparation of trioxanes 13c, 13g, and 14a,b.
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14 The treated mice surviving beyond day 28 were recorded as the mice protected by the drug. Mice treated with β-Arteether served as positive controls.
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14 The treated mice surviving beyond day 28 were recorded as the mice protected by the drug. Mice treated with β-Arteether served as positive controls.
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100% suppression of parasiteamia means that the number of parasites, if at all present, are below the detection limit. The parasites present below the detection limit can multiply and eventually can be detected. In such cases though the drug is providing near 100% suppression of the parasiteamia but will not provide full protection to the treated mice. Multidrug resistant Plasmodium yoelii nigeriensis used in this study is resistant to chloroquine. mefloquine and halofantrine.
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(a) 100% suppression of parasiteamia means that the number of parasites, if at all present, are below the detection limit. The parasites present below the detection limit can multiply and eventually can be detected. In such cases though the drug is providing near 100% suppression of the parasiteamia but will not provide full protection to the treated mice. Multidrug resistant Plasmodium yoelii nigeriensis used in this study is resistant to chloroquine. mefloquine and halofantrine.
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100% protection means all the treated mice survive till day 28. Similarly, 50% and 20% protection means only 50% and 20% of the treated mice survive to day 28.
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(b) 100% protection means all the treated mice survive till day 28. Similarly, 50% and 20% protection means only 50% and 20% of the treated mice survive to day 28.
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5 parasitized RBC, and treatment was initiated when the parasiteamia level reached above 0.5%. Trioxane 13f was dissolved in groundnut oil and administered 10 mg/kg x 4 days by oral/intramuscular routes and 20 mg/kg x 4 days by oral route. The blood smears from the treated monkeys were examined once daily to record parasiteamia clearance time and subsequent recurrence of parasiteamia.
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5 parasitized RBC, and treatment was initiated when the parasiteamia level reached above 0.5%. Trioxane 13f was dissolved in groundnut oil and administered 10 mg/kg x 4 days by oral/intramuscular routes and 20 mg/kg x 4 days by oral route. The blood smears from the treated monkeys were examined once daily to record parasiteamia clearance time and subsequent recurrence of parasiteamia.
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