The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.

Treatment and control of schistosomiasis depends on a single drug, praziquantel, but this is not ideal for several reasons including lack of potency against the juvenile stage of the parasite, dose size, and risk of resistance. We have optimised the properties of a series of compounds we discovered...

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Main Authors:	J Mark F Gardner, Nuha R Mansour, Andrew S Bell, Helena Helmby, Quentin Bickle
Format:	Article
Language:	English
Published:	Public Library of Science (PLoS) 2021-07-01
Series:	PLoS Neglected Tropical Diseases
Online Access:	https://doi.org/10.1371/journal.pntd.0009490

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spelling	doaj-7da0507681ce4b879d1f9d9c0948fc222021-08-04T04:32:08ZengPublic Library of Science (PLoS)PLoS Neglected Tropical Diseases1935-27271935-27352021-07-01157e000949010.1371/journal.pntd.0009490The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.J Mark F GardnerNuha R MansourAndrew S BellHelena HelmbyQuentin BickleTreatment and control of schistosomiasis depends on a single drug, praziquantel, but this is not ideal for several reasons including lack of potency against the juvenile stage of the parasite, dose size, and risk of resistance. We have optimised the properties of a series of compounds we discovered through high throughput screening and have designed candidates for clinical development. The best compounds demonstrate clearance of both juvenile and adult S. mansoni worms in a mouse model of infection from a single oral dose of < 10 mg/kg. Several compounds in the series are predicted to treat schistosomiasis in humans across a range of species with a single oral dose of less than 5 mg/kg.https://doi.org/10.1371/journal.pntd.0009490
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	J Mark F Gardner Nuha R Mansour Andrew S Bell Helena Helmby Quentin Bickle
spellingShingle	J Mark F Gardner Nuha R Mansour Andrew S Bell Helena Helmby Quentin Bickle The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species. PLoS Neglected Tropical Diseases
author_facet	J Mark F Gardner Nuha R Mansour Andrew S Bell Helena Helmby Quentin Bickle
author_sort	J Mark F Gardner
title	The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.
title_short	The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.
title_full	The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.
title_fullStr	The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.
title_full_unstemmed	The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.
title_sort	discovery of a novel series of compounds with single-dose efficacy against juvenile and adult schistosoma species.
publisher	Public Library of Science (PLoS)
series	PLoS Neglected Tropical Diseases
issn	1935-2727 1935-2735
publishDate	2021-07-01
description	Treatment and control of schistosomiasis depends on a single drug, praziquantel, but this is not ideal for several reasons including lack of potency against the juvenile stage of the parasite, dose size, and risk of resistance. We have optimised the properties of a series of compounds we discovered through high throughput screening and have designed candidates for clinical development. The best compounds demonstrate clearance of both juvenile and adult S. mansoni worms in a mouse model of infection from a single oral dose of < 10 mg/kg. Several compounds in the series are predicted to treat schistosomiasis in humans across a range of species with a single oral dose of less than 5 mg/kg.
url	https://doi.org/10.1371/journal.pntd.0009490
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The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.

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