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Development of Praziquantel sulphonamide derivatives as antischistosomal drugs
The almost empty armamentarium to treat schistosomiasis, a neglected parasitic disorder caused by trematode flatworms of the genus Schistosoma, except Praziquantel (PZQ), urged to find new alternatives to fight this infection. Carbonic Anhydrase from Schistosoma mansoni (SmCA) is a possible new targ...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9154761/ https://www.ncbi.nlm.nih.gov/pubmed/35635137 http://dx.doi.org/10.1080/14756366.2022.2078970 |
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author | Angeli, Andrea Ferraroni, Marta Carta, Fabrizio Häberli, Cécile Keiser, Jennifer Costantino, Gabriele Supuran, Claudiu T. |
author_facet | Angeli, Andrea Ferraroni, Marta Carta, Fabrizio Häberli, Cécile Keiser, Jennifer Costantino, Gabriele Supuran, Claudiu T. |
author_sort | Angeli, Andrea |
collection | PubMed |
description | The almost empty armamentarium to treat schistosomiasis, a neglected parasitic disorder caused by trematode flatworms of the genus Schistosoma, except Praziquantel (PZQ), urged to find new alternatives to fight this infection. Carbonic Anhydrase from Schistosoma mansoni (SmCA) is a possible new target against this nematode. Here, we propose new PZQ derivatives bearing a primary sulphonamide group in order to obtain hybrid drugs. All compounds were evaluated for their inhibition profiles on both humans and Schistosoma CAs, X-ray crystal data of SmCA and hCA II in adduct with some inhibitors were obtained allowing the understanding of the main structural factors responsible of activity. The compounds showed in vitro inhibition of immature and adult S. mansoni, but further optimisation is required for improved activity. |
format | Online Article Text |
id | pubmed-9154761 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-91547612022-06-01 Development of Praziquantel sulphonamide derivatives as antischistosomal drugs Angeli, Andrea Ferraroni, Marta Carta, Fabrizio Häberli, Cécile Keiser, Jennifer Costantino, Gabriele Supuran, Claudiu T. J Enzyme Inhib Med Chem Research Papers The almost empty armamentarium to treat schistosomiasis, a neglected parasitic disorder caused by trematode flatworms of the genus Schistosoma, except Praziquantel (PZQ), urged to find new alternatives to fight this infection. Carbonic Anhydrase from Schistosoma mansoni (SmCA) is a possible new target against this nematode. Here, we propose new PZQ derivatives bearing a primary sulphonamide group in order to obtain hybrid drugs. All compounds were evaluated for their inhibition profiles on both humans and Schistosoma CAs, X-ray crystal data of SmCA and hCA II in adduct with some inhibitors were obtained allowing the understanding of the main structural factors responsible of activity. The compounds showed in vitro inhibition of immature and adult S. mansoni, but further optimisation is required for improved activity. Taylor & Francis 2022-05-29 /pmc/articles/PMC9154761/ /pubmed/35635137 http://dx.doi.org/10.1080/14756366.2022.2078970 Text en © 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Papers Angeli, Andrea Ferraroni, Marta Carta, Fabrizio Häberli, Cécile Keiser, Jennifer Costantino, Gabriele Supuran, Claudiu T. Development of Praziquantel sulphonamide derivatives as antischistosomal drugs |
title | Development of Praziquantel sulphonamide derivatives as antischistosomal drugs |
title_full | Development of Praziquantel sulphonamide derivatives as antischistosomal drugs |
title_fullStr | Development of Praziquantel sulphonamide derivatives as antischistosomal drugs |
title_full_unstemmed | Development of Praziquantel sulphonamide derivatives as antischistosomal drugs |
title_short | Development of Praziquantel sulphonamide derivatives as antischistosomal drugs |
title_sort | development of praziquantel sulphonamide derivatives as antischistosomal drugs |
topic | Research Papers |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9154761/ https://www.ncbi.nlm.nih.gov/pubmed/35635137 http://dx.doi.org/10.1080/14756366.2022.2078970 |
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