Synthesis and evaluation of antimicrobial activity of novel hydrazino and N-benzylidinehydrazino-substituted 4,8-dihydro-1H,3H-pyrimido[4,5-d]pyrimidin-2,7-dithiones.

A number of novel pyrimido[4,5-d]pyrimidine-2,7-dithone derivatives bearing hydrazino and N-benzylidinehydrazino substitution were efficiently synthesized and screened for in vitro antibacterial activities against the representative panel of three Gram-positive and two Gram-negative bacteria. All the synthesized compounds showed the potent inhibitory action against Gram-positive bacteria. Particularly, N-benzylidinehydrazino-substituted compounds imparted profound effect. Furthermore, the Connolly-accessible surface area values were also calculated for the target compounds and correlated with the expressed biological activity.