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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Autores principales:	J Mark F Gardner, Nuha R Mansour, Andrew S Bell, Helena Helmby, Quentin Bickle
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2021
Materias:	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270
Acceso en línea:	https://doaj.org/article/7da0507681ce4b879d1f9d9c0948fc22
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spelling	oai:doaj.org-article:7da0507681ce4b879d1f9d9c0948fc222021-11-25T06:33:29ZThe discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species.1935-27271935-273510.1371/journal.pntd.0009490https://doaj.org/article/7da0507681ce4b879d1f9d9c0948fc222021-07-01T00:00:00Zhttps://doi.org/10.1371/journal.pntd.0009490https://doaj.org/toc/1935-2727https://doaj.org/toc/1935-2735Treatment 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.J Mark F GardnerNuha R MansourAndrew S BellHelena HelmbyQuentin BicklePublic Library of Science (PLoS)articleArctic medicine. Tropical medicineRC955-962Public aspects of medicineRA1-1270ENPLoS Neglected Tropical Diseases, Vol 15, Iss 7, p e0009490 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270
spellingShingle	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 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.
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.
format	article
author	J Mark F Gardner Nuha R Mansour Andrew S Bell Helena Helmby Quentin Bickle
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)
publishDate	2021
url	https://doaj.org/article/7da0507681ce4b879d1f9d9c0948fc22
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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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