title: Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT.
abstract: 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.
authors.affiliation: Strathclyde Institute for Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow G4 0RE, UK.
authors.forename: Rachel L
authors.initials: RL
authors.lastname: Clark
authors.forename: Carol J
authors.initials: CJ
authors.lastname: Clements
authors.forename: Michael P
authors.initials: MP
authors.lastname: Barrett
authors.forename: Simon P
authors.initials: SP
authors.lastname: Mackay
authors.forename: Rajendra P
authors.initials: RP
authors.lastname: Rathnam
authors.forename: George
authors.initials: G
authors.lastname: Owusu-Dapaah
authors.forename: John
authors.initials: J
authors.lastname: Spencer
authors.forename: Judith K
authors.initials: JK
authors.lastname: Huggan
mesh_terms: D000818:Animals; D001569:Benzodiazepines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008826:Microbial Sensitivity Tests; D011799:Quinazolines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy
chemical_list: D011799:Quinazolines; D014344:Trypanocidal Agents; D001569:Benzodiazepines