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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.