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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...

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Autores principales: Dolensky, Johanna, Hinteregger, Clemens, Leitner, Andreas, Seebacher, Werner, Saf, Robert, Belaj, Ferdinand, Mäser, Pascal, Kaiser, Marcel, Weis, Robert
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
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.
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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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