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

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 (ID50) of less than 50 nM and therapeutic indices (TI) up to 4000 were observed. (C) 2012 Elsevier Ltd. All rights reserved.