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The Structure–Photosynthesis-Inhibiting Activity Relationships of the Compounds Containing the N-Arylpiperazine Moiety
* 1 , 2 , 3 , 1 , 2
1  Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University in Bratislava, Odbojárov 10, SK-832 32 Bratislava, Slovak Republic
2  Institute of Chemistry, Faculty of Natural Sciences, Comenius University in Bratislava, Mlynská dolina Ch-2, Ilkovičova Str. 6, SK-842 15 Bratislava, Slovak Republic
3  Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences in Brno, Palackého 1946/1, CZ-612 42 Brno, Czech Republic


The research was focused on in silico characterization and in vitro biological testing of the series of the compounds carrying a N-arylpiperazine scaffold. Their in silico investigation was based on the prediction of electronic, steric and lipohydrophilic features. The in vitro inhibitory impact of those molecules on a photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts was evaluated using the Hill reaction. Among the tested N-arylpiperazines, the most promising potential to inhibit the PET was found for 1-[3-(3-ethoxyphenyl- carbamoyl)oxy-2-hydroxypropyl]-4-(3-trifluoromethylphenyl)piperazin-1-ium chloride and 1-[3-(4-ethoxyphenylcarbamoyl)oxy-2-hydroxypropyl]-4-(3-trifluoromethylphenyl)piperazin-1-ium chloride. The current study discussed preliminary structure–photosynthesis-inhibiting activity relationships considering electronic, steric and lipophilic properties.

Keywords: N-Arylpiperazines; Photosynthesis Inhibition; Electronic Properties; Lipophilicity.