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

Petritsch, M. and Seebacher, W. and Mohsin, N. U. and Dolensky, J. and Hochegger, P. and Kaiser, M. and Mäser, P. and Belaj, F. and Saf, R. and Kretschmer, N. and Alajlani, M. and Brantner, A. and Bauer, R. and Schuhly, W. and Weis, R.. (2021) Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities. Eur J Med Chem, 210. p. 112969.

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Official URL: https://edoc.unibas.ch/89301/

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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.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel and Mäser, Pascal
Item Type:Article, refereed
Article Subtype:Research Article
ISSN:1768-3254 (Electronic)0223-5234 (Linking)
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:20 Dec 2022 15:16
Deposited On:20 Dec 2022 15:16

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