title: Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity.
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.
authors.affiliation: School of Science, University of Greenwich at Medway, Chatham, UK. j.spencer@gre.ac.uk
authors.forename: John
authors.initials: J
authors.lastname: Spencer
authors.forename: Rajendra P
authors.initials: RP
authors.lastname: Rathnam
authors.forename: Alan L
authors.initials: AL
authors.lastname: Harvey
authors.forename: Carol J
authors.initials: CJ
authors.lastname: Clements
authors.forename: Rachel L
authors.initials: RL
authors.lastname: Clark
authors.forename: Michael P
authors.initials: MP
authors.lastname: Barrett
authors.forename: Pui Ee
authors.initials: PE
authors.lastname: Wong
authors.forename: Louise
authors.initials: L
authors.lastname: Male
authors.forename: Simon J
authors.initials: SJ
authors.lastname: Coles
authors.forename: Simon P
authors.initials: SP
authors.lastname: Mackay
mesh_terms: D001569:Benzodiazepines / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D014344:Trypanocidal Agents; D001569:Benzodiazepines