In this study, we report a novel imine derivatives synthesis (A and B) by reacting pure amoxicillin drugs with 2-aminobenzaldehyde and 2-methylbenzaldehyde. Spectroscopic techniques, such as FT‐IR spectroscopy, characterized the derivatives (A and B). All the synthesized derivatives (A and B) were evaluated in vitro against microorganisms such as Bacillus subtilis and E. coli by zone inhibition method and screened for antimicrobial activities and anti-breast cancer MCF-7 cell viability cell lines.