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

Bogdana Krivogorsky; Jennifer A. Pernat; Kelsi A. Douglas; Nikolas J. Czerniecki; Peter Grundt

doi:10.1016/j.bmcl.2012.02.038

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

Bogdana Krivogorsky
, Jennifer A. Pernat
, Kelsi A. Douglas
, Nikolas J. Czerniecki
, Peter Grundt

Chemistry & Biochemistry

Research output: Contribution to journal › Article › peer-review

24 Scopus citations

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.

Original language	English (US)
Pages (from-to)	2980-2982
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2012.02.038
State	Published - Apr 15 2012

Bibliographical note

Funding Information:
Funds for this work were provided by the University of Minnesota Undergraduate Research Opportunity Program and the Swenson Family. We also acknowledge Matthew Rodstein for critically reading an earlier version of this manuscript.

Copyright:
Copyright 2012 Elsevier B.V., All rights reserved.

Keywords

Antiparasitic activity
Berberine
Toxoplasma gondii

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10.1016/j.bmcl.2012.02.038

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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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AU - Pernat, Jennifer A.

AU - Douglas, Kelsi A.

AU - Czerniecki, Nikolas J.

AU - Grundt, Peter

N1 - Funding Information: Funds for this work were provided by the University of Minnesota Undergraduate Research Opportunity Program and the Swenson Family. We also acknowledge Matthew Rodstein for critically reading an earlier version of this manuscript. Copyright: Copyright 2012 Elsevier B.V., All rights reserved.

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AB - 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.

KW - Antiparasitic activity

KW - Berberine

KW - Toxoplasma gondii

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ER -

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

Abstract

Bibliographical note

Keywords

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