Next Article in Journal
An Unsymmetrical Tetrathiafulvalene with a Fused 1,2,5-Thiadiazole Ring and Methylthio Groups
Previous Article in Journal
Soft Alkyl Ether Prodrugs of a Model Phenolic Drug: The Effect of Incorporation of Ethyleneoxy Groups on Transdermal Delivery
Article Menu

Article Versions

Export Article

Open AccessArticle
Molecules 2009, 14(10), 4246-4265; doi:10.3390/molecules14104246

Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues

1
Zentiva k.s., U kabelovny 130, 102 37 Prague 10, Czech Republic
2
Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1-3, 612 42 Brno, Czech Republic
3
Institute of Chemistry, University of Silesia, Szkolna 9, 40007 Katowice, Poland
4
Department of Ecosozology and Physiotactics, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia
5
Department of Biological Sciences, Cork Institute of Technology, Bishopstown, Cork, Ireland
6
Institute of Chemistry, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia
7
Department of Biological and Medical Sciences, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
*
Author to whom correspondence should be addressed.
Received: 21 September 2009 / Revised: 13 October 2009 / Accepted: 21 October 2009 / Published: 23 October 2009
Download PDF [194 KB, uploaded 18 June 2014]

Abstract

In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.
Keywords: styrylquinazolinone and styrylquinazoline derivatives; lipophilicity; PET inhibition; spinach chloroplasts; in vitro antimycobacterial activity; in vitro antifungal activity; structure-activity relationships styrylquinazolinone and styrylquinazoline derivatives; lipophilicity; PET inhibition; spinach chloroplasts; in vitro antimycobacterial activity; in vitro antifungal activity; structure-activity relationships
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Jampilek, J.; Musiol, R.; Finster, J.; Pesko, M.; Carroll, J.; Kralova, K.; Vejsova, M.; O'Mahony, J.; Coffey, A.; Dohnal, J.; Polanski, J. Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues. Molecules 2009, 14, 4246-4265.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top