The reaction of β-dicarbonyl compounds as ethyl acetoacetate with hydrazines is a well-established route for the creation of pyrazole derivatives. In this research, 4-hydrazinoquinazoline (4) reacted with ethyl acetoacetate in boiling ethanol it gives ethyl 3-oxobutanoate quinazolin-4-yl-hydrazone (5). Cyclization of the compound (5) in the presence of glacial acetic acid is passed to form 4-(5-hydroxy-3-methyl-1H-pyrazol-1-yl)quinazoline(6). Furthermore, the reaction of phenylisothiocyanate compounds with hydrazines is a well-established way for the synthesis of tetrazinoquinazoline (8). The new compounds are confirmed by elemental analysis, nuclear magnetic resonance, infrared, and mass spectra. In-vitro anti-tumor evaluation of the new compounds across three cell lines HepG2 (liver carcinoma), HCT-116 (colon carcinoma), and MCF-7 (breast carcinoma) indicats high anti-tumor activity. In addition, antimicrobial activity of specific synthesized compounds are screened against four bacterial species. Amongst four, two Gram-negative are Escherichia coli, Pseudomonas aeuroginosa and gram-positive as Staphylococcus aureus and Bacillus subtilis. The antibacterial activity of Compounds (5) and (6) are greater comparing to standard drug (Amphicillin).


Fatma A. M. Mohamed, Bi Bi Zainab Mazhari, Mona F. Warrad, Hesham A. M. Gomaa, Asmaa T. Ali, Shaimaa Salah Eldeen Hussein and Hendawy Om