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Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity
Journal article   Peer reviewed

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

John Spencer, Rajendra P. Rathnam, Alan L. Harvey, Carol J. Clements, Rachel L. Clark, Michael P. Barrett, Pui Ee Wong, Louise Male, Simon J. Coles and Simon P. Mackay
Bioorganic & medicinal chemistry, Vol.19(5), pp.1802-1815
01/03/2011
DOI: https://doi.org/10.1016/j.bmc.2011.01.010
PMID: 21306904

Abstract

Biochemistry & Molecular Biology Chemistry Chemistry, Medicinal Chemistry, Organic Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology
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 mu M. (C) 2011 Elsevier Ltd. All rights reserved.

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