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Structure-activity studies of some berberine analogs as inhibitors of Toxoplasma gondii

Bogdana Krivogorsky¹, Jennifer A Pernat, Kelsi A Douglas

¹Department of Chemistry & Biochemistry, University of Minnesota Duluth, Duluth, MN 55812, United States.

Bioorganic & Medicinal Chemistry Letters

|March 20, 2012

Abstract:

The shortfalls of the current treatment options against infections with the parasite Toxoplasma gondii (T. gondii) necessitates the development of non-toxic and well-tolerated alternatives. To address this problem a structurally diverse panel of berberine alkaloids was synthesized and evaluated for in vitro inhibition of T. gondii tachyzoites. Inhibitory doses (ID(50)) of less than 50 nM and therapeutic indices (TI) up to 4000 were observed.

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