Cytotoxicity and Antimicrobial Activities of Dihydropyrimidine Derivatives Containing Pyrrole

Given the important role that heterocyclic compounds play in the pharmaceutical and medical industries; it is essential to understand their unique properties. In particular, the presence of two heterocyclic rings in these compounds enhances their biological activity and makes them valuable in various therapeutic applications. Numerous studies have shown that heterocyclic compounds derived from pyrimidine and pyrrole exhibit various biological activities, including antimicrobial, antifungal, antiviral, and antitumor properties. Therefore, this study aims to evaluate the antimicrobial and anticancer effects of synthetic compounds on several Gram-positive and Gram-negative bacteria, as well as normal and cancerous breast cell lines, in vitro.

In this experimental study, ten derivatives of dihydropyrimidine compounds attached to pyrrole were synthesized. The antibacterial activity of these compounds was evaluated against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis, and compared with gentamicin and ciprofloxacin. Their anticancer activity was assessed in a breast cancer cell line, compared with doxorubicin, at 48 and 72 hours using an MTT assay to determine cytotoxicity.

Among these compounds, compound 4e, which contains chlorine, exhibited the highest antimicrobial effect, with MIC= 3.90 μg/ml and MBC= 7.81 μg/ml, compared to gentamicin, which had MIC= 0.031 μg/ml and MBC= 0.125 μg/ml. Also, compound 4e demonstrated the highest inhibitory effect, with IC₅₀= 0.16 ± 0.009 μM, compared to doxorubicin (IC₅₀= 3.42 ± 0.10 μM), which was used as the reference drug after 48 hours.

The results of this research demonstrated the effectiveness of synthetic compounds against Gram-positive bacteria and cancer cells. These findings suggest that these compounds shave the potential to serve as effective antimicrobial and anticancer agents.