New orally active artemisinin dimer antimalarials

• Main Authors: Mahmoud A ElSohly, Waseem Gul, Shabana I Khan, Babu L Tekwani
• Format: Article
• Language: English
• Published: Wolters Kluwer Medknow Publications 2017-01-01
• Series: World Journal of Traditional Chinese Medicine
• Subjects: Artemisinin; Artemisinin dimer; Plasmodium berghei; Plasmodium falciparum
• Online Access: http://www.wjtcm.net/article.asp?issn=2311-8571;year=2017;volume=3;issue=3;spage=1;epage=11;aulast=ElSohly
• ISSN: 2311-8571; 2589-2894

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).