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Toward more drug like inhibitors of trypanosome alternative oxidase
journal contribution
posted on 2023-06-09, 09:10 authored by Ryan West, Thomas Cunningham, Lewis Pennicott, Srinivasa Rao, Simon WardNew tools are required to ensure the adequate control of the neglected tropical disease human African trypanosomiasis. Annual reports of infection have recently fallen to fewer than 5000 cases per year; however, current therapies are hard to administer and have safety concerns and, hence, are far from ideal. Trypanosome alternative oxidase is an exciting target for controlling the infection; it is unique to the parasite, and inhibition of this enzyme with the natural product ascofuranone has shown to clear in vivo infections. We report the synthesis and associated structure activity relationships of inhibitors based upon this natural product with correlation to T. b. brucei growth inhibition in an attempt to generate molecules that possess improved physicochemical properties and potential for use as new treatments for human African trypanosomiasis.
History
Publication status
- Published
Journal
ACS Infectious DiseasesISSN
2373-8227Publisher
American Chemical SocietyExternal DOI
Issue
4Volume
4Page range
592-604Department affiliated with
- Chemistry Publications
Research groups affiliated with
- Sussex Drug Discovery Centre Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2018-02-06First Compliant Deposit (FCD) Date
2018-02-06Usage metrics
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