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Drug Res (Stuttg) 2019; 69(06): 337-341
DOI: 10.1055/a-0775-0737
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

In vitro Anti-Trypanosomal Activities of Indanone-Based Chalcones

Richard M. Beteck
1   Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa
,
Lesetje J. Legoabe
1   Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa
,
Michelle Isaacs
2   Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown, South Africa
,
Heinrich C. Hoppe
2   Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown, South Africa
3   Department of Biochemistry and Microbiology, Rhodes University, Grahamstown, South Africa
› Author Affiliations
Further Information

Publication History

received 30 July 2018

accepted 17 October 2018

Publication Date:
16 November 2018 (online)

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Abstract

Human African trypanosomiasis is a neglected infectious disease that affects mostly people living in the rural areas of Africa. Current treatment options are limited to just four drugs that have been in use of four to nine decades. The life-threatening toxic side-effects associated with the use of these drugs are disconcerting. Poor efficacy, low oral bioavailability, and high cost are other shortcomings of current HAT treatments. Evaluating the potentials of known hits for other therapeutic areas may be a fast and convenient method to discover new hit compounds against alternative targets. A library of 34 known indanone based chalcones was screened against T.b. brucei and nine potent hits, having IC50 values between 0.5–8.9 µM, were found. The SAR studies of this series could provide useful information in guiding future exploration of this class of compounds in search of more potent, safe, and low cost anti-trypanosomal agents. [Graphical Abstract]

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Graphical Abstract

Key words

indanones - chalcones - anti-trypanosomal - HTS - HAT
 

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