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Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

Spencer, John and Rathnam, Rajendra P. and Harvey, Alan L. and Clements, Carol J. and Clark, Rachel L. and Barrett, Michael P. and Wong, Pui Ee and Male, Louise and Coles, Simon J. and Mackay, Simon P. (2011) Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. Bioorganic and Medicinal Chemistry, 19 (5). pp. 1802-1815.

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Abstract

A library of 1,4-benzodiazepines has been synthesized and evaluated against Trypanosoma brucei, a causative parasite of Human African trypanosomiasis. Benzodiazepines possessing a P2- transporter motif were found to have MIC values as low as 0.78 μM.

Item type: Article
ID code: 31585
Notes: Copyright © 2011 Elsevier Ltd. All rights reserved.
Keywords: synthesis, biological evaluation , 1,4-benzodiazepin-2-ones , antitrypanosomal activity , parallel synthesis, trypanosoma , benzodiazepines, microwaves, Pharmacy and materia medica, Medicine(all)
Subjects: Medicine > Pharmacy and materia medica
Department: Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences > Pharmaceutical Sciences
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Depositing user: Pure Administrator
Date Deposited: 15 Jun 2011 14:45
Last modified: 27 Mar 2014 09:24
URI: http://strathprints.strath.ac.uk/id/eprint/31585

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