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

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

Spencer, John, Rathnam, Rajendra P., Harvey, Alan L., Clements, Carol J., Clark, Rachel L., Barrett, Michael P., Wong, Pui Ee, Male, Louise, Coles, Simon J. and Mackay, Simon P. (2011) Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. Bioorganic & Medicinal Chemistry, 19 (5). pp. 1802-1815. ISSN 0968-0896 (doi:10.1016/j.bmc.2011.01.010)

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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 lM.

Item Type: Article
Uncontrolled Keywords: parallel synthesis, microwaves, benzodiazepines, trypanosoma
Subjects: R Medicine > RC Internal medicine > RC0321 Neuroscience. Biological psychiatry. Neuropsychiatry
R Medicine > RM Therapeutics. Pharmacology
Faculty / School / Research Centre / Research Group: Faculty of Engineering & Science > School of Science (SCI)
Related URLs:
Last Modified: 07 Dec 2016 14:50
URI: http://gala.gre.ac.uk/id/eprint/5837

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