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The synthesis of nine new quinazoline derivatives (2a-2i) and evaluation of their antimicrobial and cytotoxic activities were aims of the present work. For the synthesis of the compounds, 2-chloro-6,7-dimethoxyquinazolin-4-amine was used as the initial starting material. The intermediate product, 2-hydrazinyl-6,7-dimethoxyquinazolin-4-amine, was reacted with appropriate aromatic aldehydes to obtain 2-(2-benzylidenehydrazinyl)-6,7-dimethoxyquinazolin-4-amine derivatives as final compounds. The structures of the compounds were elucidated by 1H- and 13C-NMR, IR, and MS analyses. The new pure compounds were evaluated for their potential antimicrobial and cytotoxic activities using in vitromicrodilution and cell culture techniques, respectively. The compounds 2eand 2fmay be promising candidates for the treatment of fungal infections with their activity and cytotoxicity.