Toward more drug like inhibitors of trypanosome alternative oxidase

West, Ryan A., Cunningham, Thomas, Pennicott, Lewis E., Rao, Srinivasa P. S. and Ward, Simon ORCID: https://orcid.org/0000-0002-8745-8377 2018. Toward more drug like inhibitors of trypanosome alternative oxidase. ACS Infectious Diseases 4 (4) , pp. 592-604. 10.1021/acsinfecdis.7b00218

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Abstract

New 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.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Medicine
Uncontrolled Keywords:	drug design; human African trypanosomiasis; medicinal chemistry; multiparameter optimization
Publisher:	American Chemical Society
ISSN:	2373-8227
Date of First Compliant Deposit:	22 February 2018
Last Modified:	28 Nov 2024 21:30
URI:	https://orca.cardiff.ac.uk/id/eprint/109254

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