Biological activity of substituted 2-aminothiobenzamides and quinazolin-4-thiones

Jiří Hanusek¹ (Jiri.Hanusek@upce.cz), Martin Šustr², Petra Kubanová³, Vladimír Buchta³, Miloš Sedlák¹

¹ Department of Organic Chemistry, Faculty of Chemical Technology, University of Pardubice, Czech Republic,
² Department of Inorganic and Organic Chemistry and ³ Department of Biological and Medical Sciences, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Czech Republic

Summary

This work is focused on the investigation of biological activity for a set of previously prepared 2-aminothiobenzamides, 2-benzoylaminothiobenzamides, 2-phenylquinazolin-4-thiones, 2,2-dimethyl-3-phenylquinazolin-4(1H,3H)-thiones, and 2-methyl-3-phenylquinazolin-4-thiones. In the groups of the open derivatives, the presence of hydrogen at 2-amino group appears to be obviously essential for the antifungal activity. The ring closure to quinazolin-4-thione derivatives mainly led to inactive products. In the groups of 2-benzoylaminothiobenzamides and quinazolin-4-thiones, antialgal and tuberculostatic effects were also tested. The substances having hydrogen at the 2-amino group show higher tuberculostatic activity than the corresponding N-methyl derivatives.