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Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores
N-(Aminoalkyl)azabicyclo[3.2.2]nonanes possess antiplasmodial and antitrypanosomal activity. A series with terminal tetrazole or sulfonamido partial structure was prepared. The structures of all new compounds were confirmed by NMR and IR spectroscopy and by mass spectral data. A single crystal struc...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9572860/ https://www.ncbi.nlm.nih.gov/pubmed/36234752 http://dx.doi.org/10.3390/molecules27196217 |
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author | Dolensky, Johanna Hinteregger, Clemens Leitner, Andreas Seebacher, Werner Saf, Robert Belaj, Ferdinand Mäser, Pascal Kaiser, Marcel Weis, Robert |
author_facet | Dolensky, Johanna Hinteregger, Clemens Leitner, Andreas Seebacher, Werner Saf, Robert Belaj, Ferdinand Mäser, Pascal Kaiser, Marcel Weis, Robert |
author_sort | Dolensky, Johanna |
collection | PubMed |
description | N-(Aminoalkyl)azabicyclo[3.2.2]nonanes possess antiplasmodial and antitrypanosomal activity. A series with terminal tetrazole or sulfonamido partial structure was prepared. The structures of all new compounds were confirmed by NMR and IR spectroscopy and by mass spectral data. A single crystal structure analysis enabled the distinction between isomers. The antiprotozoal activities were examined in vitro against strains of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). The most active sulfonamide and tetrazole derivates showed activities in the submicromolar range. |
format | Online Article Text |
id | pubmed-9572860 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-95728602022-10-17 Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores Dolensky, Johanna Hinteregger, Clemens Leitner, Andreas Seebacher, Werner Saf, Robert Belaj, Ferdinand Mäser, Pascal Kaiser, Marcel Weis, Robert Molecules Article N-(Aminoalkyl)azabicyclo[3.2.2]nonanes possess antiplasmodial and antitrypanosomal activity. A series with terminal tetrazole or sulfonamido partial structure was prepared. The structures of all new compounds were confirmed by NMR and IR spectroscopy and by mass spectral data. A single crystal structure analysis enabled the distinction between isomers. The antiprotozoal activities were examined in vitro against strains of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). The most active sulfonamide and tetrazole derivates showed activities in the submicromolar range. MDPI 2022-09-21 /pmc/articles/PMC9572860/ /pubmed/36234752 http://dx.doi.org/10.3390/molecules27196217 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Dolensky, Johanna Hinteregger, Clemens Leitner, Andreas Seebacher, Werner Saf, Robert Belaj, Ferdinand Mäser, Pascal Kaiser, Marcel Weis, Robert Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores |
title | Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores |
title_full | Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores |
title_fullStr | Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores |
title_full_unstemmed | Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores |
title_short | Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores |
title_sort | antiprotozoal activity of azabicyclo-nonanes linked to tetrazole or sulfonamide cores |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9572860/ https://www.ncbi.nlm.nih.gov/pubmed/36234752 http://dx.doi.org/10.3390/molecules27196217 |
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