Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity

A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their tyrosinase and urease inhibitory activity. Evaluation of prepared derivatives demonstrated that compounds (8b) and (8j) are mo...

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Autores principales: Mojzych, Mariusz, Tarasiuk, Paweł, Kotwica-Mojzych, Katarzyna, Rafiq, Muhammad, Seo, Sung-Yum, Nicewicz, Michał, Fornal, Emilia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2016
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6010123/
https://www.ncbi.nlm.nih.gov/pubmed/27778522
http://dx.doi.org/10.1080/14756366.2016.1238362
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author Mojzych, Mariusz
Tarasiuk, Paweł
Kotwica-Mojzych, Katarzyna
Rafiq, Muhammad
Seo, Sung-Yum
Nicewicz, Michał
Fornal, Emilia
author_facet Mojzych, Mariusz
Tarasiuk, Paweł
Kotwica-Mojzych, Katarzyna
Rafiq, Muhammad
Seo, Sung-Yum
Nicewicz, Michał
Fornal, Emilia
author_sort Mojzych, Mariusz
collection PubMed
description A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their tyrosinase and urease inhibitory activity. Evaluation of prepared derivatives demonstrated that compounds (8b) and (8j) are most potent mushroom tyrosinase inhibitors whereas all of the obtained compounds showed higher urease inhibitory activity than the standard thiourea. The compounds (8a), (8f) and (8i) exhibited excellent enzyme inhibitory activity with IC(50) 0.037, 0.044 and 0.042 μM, respectively, while IC(50) of thiourea is 20.9 μM.
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spelling pubmed-60101232018-07-11 Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity Mojzych, Mariusz Tarasiuk, Paweł Kotwica-Mojzych, Katarzyna Rafiq, Muhammad Seo, Sung-Yum Nicewicz, Michał Fornal, Emilia J Enzyme Inhib Med Chem Research Article A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their tyrosinase and urease inhibitory activity. Evaluation of prepared derivatives demonstrated that compounds (8b) and (8j) are most potent mushroom tyrosinase inhibitors whereas all of the obtained compounds showed higher urease inhibitory activity than the standard thiourea. The compounds (8a), (8f) and (8i) exhibited excellent enzyme inhibitory activity with IC(50) 0.037, 0.044 and 0.042 μM, respectively, while IC(50) of thiourea is 20.9 μM. Taylor & Francis 2016-10-25 /pmc/articles/PMC6010123/ /pubmed/27778522 http://dx.doi.org/10.1080/14756366.2016.1238362 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group http://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/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Mojzych, Mariusz
Tarasiuk, Paweł
Kotwica-Mojzych, Katarzyna
Rafiq, Muhammad
Seo, Sung-Yum
Nicewicz, Michał
Fornal, Emilia
Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
title Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
title_full Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
title_fullStr Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
title_full_unstemmed Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
title_short Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
title_sort synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6010123/
https://www.ncbi.nlm.nih.gov/pubmed/27778522
http://dx.doi.org/10.1080/14756366.2016.1238362
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