Anti-schistosomal activities of quinoxaline-containing compounds: From hit identification to lead optimisation

Padalino, Gilda, El-Sakkary, Nelly, Liu, Lawrence J., Liu, Chenxi, Harte, Danielle S.G., Barnes, Rachel E., Sayers, Edward ORCID: https://orcid.org/0000-0002-2621-1119, Forde-Thomas, Josephine, Whiteland, Helen, Bassetto, Marcella ORCID: https://orcid.org/0000-0002-2491-5868, Ferla, Salvatore, Johnson, George, Jones, Arwyn T. ORCID: https://orcid.org/0000-0003-2781-8905, Caffrey, Conor R., Chalmers, Iain, Brancale, Andrea ORCID: https://orcid.org/0000-0002-9728-3419 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
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:	12 Nov 2024 02:45
URI:	https://orca.cardiff.ac.uk/id/eprint/144330

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