Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT

A library of 1,4-benzodiazepines has been synthesised and evaluated for activity against Trypanosoma brucei, a causative parasite of Human African Trypanosomiasis (HAT). The most potent of these derivatives has an MIC value of 0.97 μM. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds.

A library of 1,4-benzodiazepines and quinazoline-2,4-diones has been synthesised that display MIC values as low as 0.97 μM against Trypanosoma brucei.Figure optionsDownload as PowerPoint slide