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

Bioorg Med Chem Lett. 2012 Feb 22. [Epub ahead of print]

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

Krivogorsky B, Pernat JA, Douglas KA, Czerniecki NJ, Grundt P.

Source
Department of Chemistry & Biochemistry, University of Minnesota Duluth, 1039 University Drive, Duluth, MN 55812, United States.

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 50nM and therapeutic indices (TI) up to 4000 were observed.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID: 22425568 [PubMed - as supplied by publisher]