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Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities

Authors :
Nadine Kretschmer
Marcel Kaiser
Muaaz Alajlani
Robert Weis
Robert Saf
Adelheid Brantner
Werner Seebacher
Rudolf Bauer
Noor-ul-Amin Mohsin
Wolfgang Schühly
Ferdinand Belaj
Johanna Dolensky
Markus Petritsch
Pascal Mäser
Patrick Hochegger
Source :
European Journal of Medicinal Chemistry. 210:112969
Publication Year :
2021
Publisher :
Elsevier BV, 2021.

Abstract

New 1,3 dibenzyl -tetrahydropyridinylidene ammonium salts have been prepared from unsubstituted or N-benzylated tetrahydropyridinylidene ammonium salts. The antiplasmodial and antitrypanosomal activities as well as their cytotoxic effects were determined using microplate assays. In addition, their activities against two gram positive and two gram negative bacteria strains and a yeast strain were examined. Furthermore, anticancer effects against two cell lines were investigated. Physicochemical parameters were calculated and structure-activity-relationships discussed. One compound showed antiplasmodial activity against a multiresistant strain of Plasmodium falciparum in subnanomolar concentration. Antitrypanosomal activities were detected in low nanomolar concentrations. A single compound was active against grampositive and gramnegative bacteria, as well as yeast. One compound inhibited the growth of a HCT cell line in low concentration.

Details

ISSN :
02235234
Volume :
210
Database :
OpenAIRE
Journal :
European Journal of Medicinal Chemistry
Accession number :
edsair.doi.dedup.....1957f76991cb1985c939c1dc96c28d33
Full Text :
https://doi.org/10.1016/j.ejmech.2020.112969