Quinazolinone derivatives bearing a trifluoromethyl substituent have attracted considerable attention. A series of novel Schiffs base, pyrazole and triazolefunctionalized quinazolinone derivatives were prepared starting from 2-amino-6-(trifluoromethyl)benzonitrile 1 on hydrolysis obtained 2- amino-6-(trifluoromethyl)benzoic acid 2, further reacts with phenylisocyanate gives 2-mercapto-3- phenyl-5-(trifluoromethyl)quinazolin-4(3H)-one 3, which upon reaction with POCl3converts to 2- chloro-3-phenyl-5-(trifluoromethyl)quinazolin-4(3H)-one 4. Further chloro derivative on reaction with hydrazinehydrate forms 2-hydrazinyl-3-phenyl-5-(trifluoromethyl)quinazolin-4(3H)-one 5. Compound 5, on further reaction with aromatic acids, 3-oxo-3-phenylpropanenitrile, and aromatic aldehydes, to get triazole, pyrazole, and Schiff's base functionalized quinazolinone derivatives 6a-d, 7a-d and 8a-d. All the final compounds evaluated for anticancer activity against four human cancer cell lines such as ‘HeLa-Cervical cancer (CCL-2); COLO 205-Colon cancer (CCL-222); HepG2-Liver cancer (HB-8065); MCF7-Breast cancer (HTB-22) and normal cell line such as HEK-293 – Human Embryonic Kidney cells (CRL-1573)’ and promising compounds which showed good activity have been identified and docking interactions are also identified. All the synthesized compounds were screened against Gram-positive and Gram-negative bacterial strains and one Candida strain by the well diffusion method. Some of the compounds showed promising antibacterial activity against bacterial strains as compared to the standards.
Junaid et al. (Mon,) studied this question.