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| New Orally Active Artemisinin Dimer Antimalarials |
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| DOI：10.4103/wjtcm.wjtcm_10_17 |
| KeyWord:Artemisinin, Artemisinin dimer, Plasmodium berghei, Plasmodium falciparum |
| Author | Institution |
| Mahmoud A. ElSohlyabc |
a.ElSohly Laboratories, Inc., 5 Industrial Park Drive, Oxford, b.National Center for Natural Products Research, Departments of c.Pharmaceutics and Drug Delivery,School of Pharmacy, The University of Mississippi, University, MS 38677, USA |
| Waseem Gulab |
a.ElSohly Laboratories, Inc., 5 Industrial Park Drive, Oxford, b.National Center for Natural Products Research, Departments of Pharmacy, The University of Mississippi, University, MS 38677,USA |
| Shabana I. Khanbd |
b.National Center for Natural Products Research, Departments of Pharmacy, The University of Mississippi, University, MS 38677,USA,d.Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA |
| Babu L. Tekwanibd |
b.National Center for Natural Products Research, Departments of Pharmacy, The University of Mississippi, University, MS 38677,USA,d.Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA |
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| Abstract: |
| Objective: To synthesize orally bioavailable artemisinin dimers and the evaluation of their in vivo antimalarial activity. Methods: Artemsisin dimers were synthesized and their antimalarial activity was determined in in vitro and in vivo studies (administered orally and IP). Results: Dimers 5 and 6 provided 100% suppression of parastemia throughout the oral administration study, with all animals surviving up to day 28 (the last day of the study). Conclusion: Dimers 4-7 displayed markedly improved in vitro activity against P. falciparum, while the in vivo activity against P. berghei was highly encouraging, with 5 and 6 completely clearing parasitemia from the start of the drug treatment until the end of the study (day 28). |
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