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ORIGINAL ARTICLE
Year : 2017  |  Volume : 3  |  Issue : 3  |  Page : 1-11

New orally active artemisinin dimer antimalarials


1 ElSohly Laboratories, Inc., 5 Industrial Park Drive, Oxford; National Center for Natural Products Research; Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA
2 ElSohly Laboratories, Inc., 5 Industrial Park Drive, Oxford; National Center for Natural Products Research, MS 38677, USA
3 National Center for Natural Products Research; Biomolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA

Correspondence Address:
Babu L Tekwani
National Center for Natural Products Research, School of Pharmacy, University of Mississippi, MS 38677
USA
Mahmoud A ElSohly
ElSohly Laboratories, Inc., 5 Industrial Park Drive, Oxford, MS 38655
USA
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/wjtcm.wjtcm_10_17

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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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