2-AZETIDINONE DERIVATIVES: SYNTHESIS, ANTIMICROBIAL, ANTICANCER EVALUATION AND QSAR STUDIES

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Pharmacology

Background:

• 2-azetidinone derivatives are recognized for diverse biological activities.
• Hippuric acid serves as a versatile starting material for synthesizing heterocyclic compounds.
• There is a continuous need for novel antimicrobial and anticancer agents.

Purpose of the Study:

• To synthesize a series of novel 2-azetidinone derivatives.
• To evaluate the in vitro antimicrobial activity against bacterial and fungal strains.
• To assess the in vitro anticancer activity against breast cancer (MCF7) cell lines.

Main Methods:

• Synthesis of 2-azetidinone derivatives using hippuric acid.
• In vitro antimicrobial assays against Gram-positive and Gram-negative bacteria and fungal strains.
• In vitro anticancer assays using breast cancer (MCF7) cell lines.
• Quantitative Structure-Activity Relationship (QSAR) modeling.

Main Results:

• Compound 4 exhibited significant antimicrobial activity.
• Compound 17 demonstrated potent anticancer activity against MCF7 cells.
• QSAR models identified topological parameters (Balaban index, molecular connectivity indices) as key determinants of antimicrobial activity.

Conclusions:

• The synthesized 2-azetidinone derivatives possess promising antimicrobial and anticancer properties.
• Specific derivatives show potential as lead compounds for further drug development.
• QSAR analysis provides insights into the structural requirements for biological activity.