Previous Article in event
Next Article in event
Substituted 2-Styrylquinazoline Derivatives: Preparation and Their Biological Activities
Published: 01 November 2009 by MDPI in The 13th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic Chemistry and Natural Products
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