The discovery of a novel series of compounds with single-dose efficacy against juvenile and adult Schistosoma species
Author(s)
Gardner, J Mark F
Mansour, Nuha R
Bell, Andrew S
Helmby, Helena
Bickle, Quentin
Type
Journal Article
Abstract
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.
Date Issued
2021-07-01
Date Acceptance
2021-05-23
Citation
PLoS Neglected Tropical Diseases, 2021, 15 (7)
ISSN
1935-2727
Publisher
Public Library of Science (PLoS)
Journal / Book Title
PLoS Neglected Tropical Diseases
Volume
15
Issue
7
Copyright Statement
Copyright: © 2021 Gardner et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
License URL
Identifier
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000677740500003&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=a2bf6146997ec60c407a63945d4e92bb
Subjects
CHEMOTHERAPY
Infectious Diseases
Life Sciences & Biomedicine
MANSONI
Parasitology
Science & Technology
Tropical Medicine
Publication Status
Published
Article Number
e0009490
Date Publish Online
2021-07-19