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Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities
- 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.
- Subjects :
- Staphylococcus aureus
Antifungal Agents
Cell Survival
Plasmodium falciparum
Antineoplastic Agents
Microbial Sensitivity Tests
01 natural sciences
Cell Line
Antimalarials
Mice
Structure-Activity Relationship
03 medical and health sciences
chemistry.chemical_compound
Parasitic Sensitivity Tests
Candida albicans
Drug Discovery
Escherichia coli
Animals
Humans
Cytotoxic T cell
Ammonium
Cell Proliferation
030304 developmental biology
Pharmacology
0303 health sciences
Dose-Response Relationship, Drug
Molecular Structure
Strain (chemistry)
biology
010405 organic chemistry
Organic Chemistry
General Medicine
Antimicrobial
biology.organism_classification
Yeast
Anti-Bacterial Agents
Rats
0104 chemical sciences
Quaternary Ammonium Compounds
chemistry
Biochemistry
Cell culture
Pseudomonas aeruginosa
Female
Salts
Drug Screening Assays, Antitumor
Epidermis
Bacteria
Subjects
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