Abstract
In this study, a series of twelve ring-substituted salicylanilides and carbamoylphenylcarbamates were prepared and characterized. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Moreover, their site of action in the photosynthetic apparatus was determined. Primary in vitro screening of the synthesized compounds was also performed against mycobacterial, bacterial and fungal strains. Several compounds showed biological activity comparable with or higher than the standards 3-(3,4-dichlorophenyl)-1,1-dimethylurea, isoniazid, penicillin G, ciprofloxacin or fluconazole. The most active compounds showed minimal anti-proliferative activity against human cells in culture, indicating they would have low cytotoxicity. For all compounds, the relationships between lipophilicity and the chemical structure are discussed.
Disciplines
Biology
DOI
10.3390/molecules15118122
Full Publication Date
November 2010
Publisher
MDPI
Resource Type
journal article
Access Rights
open access
License Condition
This work is licensed under a Creative Commons Attribution 4.0 International License.
Alternative Identifier
https://www.mdpi.com/1420-3049/15/11/8122/htm
Recommended Citation
Otevrel, J. et al., 2010. Investigating the Spectrum of Biological Activity of Ring-Substituted Salicylanilides and Carbamoylphenylcarbamates. Molecules, 15(11), pp.8122–8142. Available at: http://dx.doi.org/10.3390/molecules15118122.
Publication Details
Molecules
Copyright © 2010 Otevrei, T. et al.
This study was supported by the Ministry of Education of the Czech Republic MSM 6215712403, by the Irish Department of Education and Science TSR Strand1-06/CR08 and by Sanofi-Aventis Pharma Slovakia. D.R.R. was supported by a NHMRC Senior Principal Research Fellowship and Project grants and an ARC Discovery Grant. D.S.K. was supported by a Cancer Institute New South Wales Early Career Development Fellowship and Innovation Grant.