2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm.
The human whipworm Trichuris trichiura is a parasite that infects around 500 million people globally, with consequences including damage to physical growth and educational performance. Current drugs such as mebendazole have a notable lack of efficacy against whipworm, compared to other soil-transmit...
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Online Access: | https://doi.org/10.1371/journal.pntd.0006487 https://doaj.org/article/dbfa1530a47d45d9ab4a45f4e2a752df |
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ftdoajarticles:oai:doaj.org/article:dbfa1530a47d45d9ab4a45f4e2a752df 2023-05-15T15:06:04+02:00 2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. Frederick A Partridge Ruth Forman Nicky J Willis Carole J R Bataille Emma A Murphy Anwen E Brown Narinder Heyer-Chauhan Bruno Marinič Daniel J C Sowood Graham M Wynne Kathryn J Else Angela J Russell David B Sattelle 2018-07-01T00:00:00Z https://doi.org/10.1371/journal.pntd.0006487 https://doaj.org/article/dbfa1530a47d45d9ab4a45f4e2a752df EN eng Public Library of Science (PLoS) https://doi.org/10.1371/journal.pntd.0006487 https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0006487 https://doaj.org/article/dbfa1530a47d45d9ab4a45f4e2a752df PLoS Neglected Tropical Diseases, Vol 12, Iss 7, p e0006487 (2018) Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 article 2018 ftdoajarticles https://doi.org/10.1371/journal.pntd.0006487 2022-12-30T19:59:22Z The human whipworm Trichuris trichiura is a parasite that infects around 500 million people globally, with consequences including damage to physical growth and educational performance. Current drugs such as mebendazole have a notable lack of efficacy against whipworm, compared to other soil-transmitted helminths. Mass drug administration programs are therefore unlikely to achieve eradication and new treatments for trichuriasis are desperately needed. All current drug control strategies focus on post-infection eradication, targeting the parasite in vivo. Here we propose developing novel anthelmintics which target the egg stage of the parasite in the soil as an adjunct environmental strategy. As evidence in support of such an approach we describe the actions of a new class of anthelmintic compounds, the 2,4-diaminothieno[3,2-d]pyrimidines (DATPs). This compound class has found broad utility in medicinal chemistry, but has not previously been described as having anthelmintic activity. Importantly, these compounds show efficacy against not only the adult parasite, but also both the embryonated and unembryonated egg stages and thereby may enable a break in the parasite lifecycle. Article in Journal/Newspaper Arctic Directory of Open Access Journals: DOAJ Articles Arctic PLOS Neglected Tropical Diseases 12 7 e0006487 |
institution |
Open Polar |
collection |
Directory of Open Access Journals: DOAJ Articles |
op_collection_id |
ftdoajarticles |
language |
English |
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 Frederick A Partridge Ruth Forman Nicky J Willis Carole J R Bataille Emma A Murphy Anwen E Brown Narinder Heyer-Chauhan Bruno Marinič Daniel J C Sowood Graham M Wynne Kathryn J Else Angela J Russell David B Sattelle 2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. |
topic_facet |
Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 |
description |
The human whipworm Trichuris trichiura is a parasite that infects around 500 million people globally, with consequences including damage to physical growth and educational performance. Current drugs such as mebendazole have a notable lack of efficacy against whipworm, compared to other soil-transmitted helminths. Mass drug administration programs are therefore unlikely to achieve eradication and new treatments for trichuriasis are desperately needed. All current drug control strategies focus on post-infection eradication, targeting the parasite in vivo. Here we propose developing novel anthelmintics which target the egg stage of the parasite in the soil as an adjunct environmental strategy. As evidence in support of such an approach we describe the actions of a new class of anthelmintic compounds, the 2,4-diaminothieno[3,2-d]pyrimidines (DATPs). This compound class has found broad utility in medicinal chemistry, but has not previously been described as having anthelmintic activity. Importantly, these compounds show efficacy against not only the adult parasite, but also both the embryonated and unembryonated egg stages and thereby may enable a break in the parasite lifecycle. |
format |
Article in Journal/Newspaper |
author |
Frederick A Partridge Ruth Forman Nicky J Willis Carole J R Bataille Emma A Murphy Anwen E Brown Narinder Heyer-Chauhan Bruno Marinič Daniel J C Sowood Graham M Wynne Kathryn J Else Angela J Russell David B Sattelle |
author_facet |
Frederick A Partridge Ruth Forman Nicky J Willis Carole J R Bataille Emma A Murphy Anwen E Brown Narinder Heyer-Chauhan Bruno Marinič Daniel J C Sowood Graham M Wynne Kathryn J Else Angela J Russell David B Sattelle |
author_sort |
Frederick A Partridge |
title |
2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. |
title_short |
2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. |
title_full |
2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. |
title_fullStr |
2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. |
title_full_unstemmed |
2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. |
title_sort |
2,4-diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm. |
publisher |
Public Library of Science (PLoS) |
publishDate |
2018 |
url |
https://doi.org/10.1371/journal.pntd.0006487 https://doaj.org/article/dbfa1530a47d45d9ab4a45f4e2a752df |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
PLoS Neglected Tropical Diseases, Vol 12, Iss 7, p e0006487 (2018) |
op_relation |
https://doi.org/10.1371/journal.pntd.0006487 https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0006487 https://doaj.org/article/dbfa1530a47d45d9ab4a45f4e2a752df |
op_doi |
https://doi.org/10.1371/journal.pntd.0006487 |
container_title |
PLOS Neglected Tropical Diseases |
container_volume |
12 |
container_issue |
7 |
container_start_page |
e0006487 |
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1766337733205164032 |