Events The 13th International Electronic Conference on Synthetic Organic Chemistry

Event submissions

Published

This submission belongs to the session c. Bioorganic Chemistry and Natural Products of the event The 13th International Electronic Conference on Synthetic Organic Chemistry

Published date

01 Nov, 2009

Citation

Jaroslaw Polanski, Aidan Coffey, Jim O'Mahony, Jacek Finster, Katarina Kralova, James Carroll, Matus Pesko, Josef Jampilek, Robert Musiol, Substituted 2-Styrylquinazoline Derivatives: Preparation and Their Biological Activities, in Proceedings of The 13th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2009, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-13-00204

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Substituted 2-Styrylquinazoline Derivatives: Preparation and Their Biological Activities

Jaroslaw Polanski ¹

Aidan Coffey ²

Jim O'Mahony ²

Jacek Finster ¹

Katarina Kralova ³

James Carroll ²

Matus Pesko ⁴

Josef Jampilek ^5,6

Robert Musiol ¹

1. Institute of Chemistry, University of Silesia, Szkolna 9, 40007 Katowice, Poland

2. Department of Biological Sciences, Cork Institute of Technology, Bishopstown, Cork, Ireland

3. Institute of Chemistry, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia

4. Department of Ecosozology and Physiotactics, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia

5. Zentiva a.s., U kabelovny 130, 102 37 Prague 10, Czech Republic

6. Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 61242 Brno, Czech Republic

Abstract

In this study, a series of five ring-substituted 2-styrylquinazolin-4(3H)-one and five ring-substituted 4-chloro-2-styrylquinazoline derivatives were prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to inhibition of 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. Several compounds showed biological activity comparable with or higher than the standard isoniazid. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed, as well as their structure-activity relationships (SAR).

Keywords

Styrylquinazoline derivatives

Lipophilicity

PET inhibition

Spinach chloroplasts

In vitro antimycobacterial activity

Structure-activity relationships

STUDIES ON THE USE OF NAPHTYRIDINE DERIVATIVES AS EFFECTIVE RECEPTORS

Exact structure of bacteriophage T4 and infection: Stopping Escherichia coli