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2,4-diaminothienopyrimidines as orally active antimalarial agents

González Cabrera, Diego and Le Manach, Claire and Douelle, Frederic and Younis, Yassir and Feng, Tzu-Shean and Paquet, Tanya and Nchinda, Aloysius T. and Street, Leslie J. and Taylor, Dale and de Kock, Carmen and Wiesner, Lubbe and Duffy, Sandra and White, Karen L. and Zabiulla, K. Mohammed and Sambandan, Yuvaraj and Bashyam, Sridevi and Waterson, David and Witty, Michael J. and Charman, Susan A. and Avery, Vicky M. and Wittlin, Sergio and Chibale, Kelly. (2014) 2,4-diaminothienopyrimidines as orally active antimalarial agents. Journal of medicinal chemistry, 57 (3). pp. 1014-1022.

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Official URL: http://edoc.unibas.ch/dok/A6243433

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Abstract

A novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure-activity relationship studies identified compounds with potent antiplasmodial activity and low in vitro cytotoxicity. Several of these analogues exhibited in vivo activity in the Plasmodium berghei mouse model when administered orally. However, inhibition of the hERG potassium channel was identified as a liability for this series.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wittlin, Sergio
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:20 Oct 2017 06:28
Deposited On:18 Jul 2014 09:10

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