Beschreibung:
<jats:p>A new series of thiopyrimidine‐5‐carbonitrile derivatives were synthesized and the chemical identity of them was established on the basis of spectral methods. The antimicrobial properties of all derivatives were investigated against Gram‐positive and Gram‐negative bacteria as well as fungal strains. The results of the antimicrobial screening showed that compounds <jats:bold>4</jats:bold>, <jats:bold>11</jats:bold>, and <jats:bold>12</jats:bold> have a higher and broad spectrum efficacy against all the tested organisms in comparison with the reference drugs. Interestingly, the most active compounds <jats:bold>4</jats:bold> and <jats:bold>12</jats:bold> showed good binding assay results with <jats:styled-content style="fixed-case"><jats:italic>Escherichia coli</jats:italic></jats:styled-content> DNA gyrase comparable to that of the reference, methotrexate. Furthermore, a molecular docking study of these compounds was carried out to investigate their binding pattern with the target, DNA gyrase.</jats:p>