Padalino, Gilda, El-Sakkary, Nelly, Liu, Lawrence J., Liu, Chenxi, Harte, Danielle S.G., Barnes, Rachel E., Sayers, Edward, Forde-Thomas, Josephine, Whiteland, Helen, Bassetto, Marcella, Ferla, Salvatore, Johnson, George, Jones, Arwyn T., Caffrey, Conor R., Chalmers, Iain, Brancale, Andrea and Hoffmann, Karl F.
2021.
Anti-schistosomal activities of quinoxaline-containing compounds: From hit identification to lead optimisation.
European Journal of Medicinal Chemistry
226
, 113823.
10.1016/j.ejmech.2021.113823
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Abstract
Schistosomiasis is a neglected disease of poverty that is caused by infection with blood fluke species contained within the genus Schistosoma. For the last 40 years, control of schistosomiasis in endemic regions has predominantly been facilitated by administration of a single drug, praziquantel. Due to limitations in this mono-chemotherapeutic approach for sustaining schistosomiasis control into the future, alternative anti-schistosomal compounds are increasingly being sought by the drug discovery community. Herein, we describe a multi-pronged, integrated strategy that led to the identification and further exploration of the quinoxaline core as a promising anti-schistosomal scaffold.
Item Type: | Article |
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Date Type: | Publication |
Status: | Published |
Schools: | Pharmacy |
Publisher: | Elsevier |
ISSN: | 0223-5234 |
Date of First Compliant Deposit: | 22 September 2021 |
Date of Acceptance: | 27 August 2021 |
Last Modified: | 11 Oct 2021 16:56 |
URI: | https://orca.cardiff.ac.uk/id/eprint/144330 |
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