Structure–Activity Relationships of Synthetic Cordycepin Analogues as Experimental Therapeutics for African Trypanosomiasis

SK Vodnala, T Lundbäck, E Yeheskieli, B Sjöberg…

文献索引：Vodnala, Suman K.; Lundbaeck, Thomas; Yeheskieli, Esther; Sjoeberg, Birger; Gustavsson, Anna-Lena; Svensson, Richard; Olivera, Gabriela C.; Eze, Anthonius A.; De Koning, Harry P.; Hammarstroem, Lars G. J.; Rottenberg, Martin E. Journal of Medicinal Chemistry, 2013 , vol. 56, # 24 p. 9861 - 9873

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被引用次数: 10

摘要

ABSTRACT: Novel methods for treatment of African trypanosomiasis, caused by infection with Trypanosoma brucei are needed. Cordycepin (3′-deoxyadenosine, 1a) is a powerful trypanocidal compound in vitro but is ineffective in vivo because of rapid metabolic degradation by adenosine deaminase (ADA). We elucidated the structural moieties of cordycepin required for trypanocidal activity and designed analogues that retained ...