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Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of hat
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posted on 2023-06-08, 18:34 authored by Rachel L Clark, Carol J Clements, Michael P Barrett, Simon P Mackay, Rajendra P Rathnam, George Owusu-Dapaah, John SpencerJohn Spencer, Judith K HugganA 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.
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Publication status
- Published
Journal
Bioorganic and Medicinal ChemistryISSN
0968-0896Publisher
ElsevierExternal DOI
Issue
20Volume
20Page range
6019-6033Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2014-09-30Usage metrics
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