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

…, AL Harvey, CJ Clements, RL Clark, MP Barrett…

Index: 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.; MacKay, Simon P. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 5 p. 1802 - 1815

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Citation Number: 20

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.