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

John Spencer,Rajendra P. Rathnam,Alan L. Harvey,Carol Clements,Rachel L. Clark,Michael P. Barrett,Pui Ee Wong,Louise Male,Simon J. Coles,Simon P. Mackay

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

2011

John Spencer
Rajendra P. Rathnam
Alan L. Harvey
Carol Clements
Rachel L. Clark
Michael P. Barrett
Pui Ee Wong
Louise Male
Simon J. Coles
Simon P. Mackay

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.

Keywords:

Trypanosoma brucei
African trypanosomiasis
Chemical synthesis
Kinetoplastida
Trypanosoma
Transporter
Lactam
Stereochemistry
Biochemistry
In vitro
Chemistry

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