New Benzofuran-Pyrazole-Based Compounds as Promising Antimicrobial Agents: Design, Synthesis, DNA Gyrase B...

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Antimicrobial Drug Discovery

Background:

• Antibiotic resistance is a growing global health threat.
• Novel antimicrobial agents are urgently needed.
• Benzofuran-pyrazole scaffolds are explored for therapeutic potential.

Purpose of the Study:

• Design, synthesize, and evaluate novel benzofuran-pyrazole hybrid molecules.
• Assess their antimicrobial, antioxidant, and anti-inflammatory activities.
• Investigate their potential as DNA gyrase B inhibitors.

Main Methods:

• Synthesis of benzofuran-pyrazole hybrids via Vilsmeier-Haach reaction.
• Structural confirmation using micro-analytical and spectral techniques.
• Evaluation of antimicrobial, antioxidant, and anti-inflammatory assays, including DNA gyrase B inhibition.

Main Results:

• Compounds 9, 10, 11b-d displayed broad-spectrum antimicrobial activity (MIC 2.50–20 µg/mL).
• Compounds 4, 6, 9, 11b, 11d showed high antioxidant capacity (84.16–90.52% DPPH scavenging).
• Significant anti-inflammatory effects observed (86.70–99.25% HRBC stabilization); Compound 9 inhibited E. coli DNA gyrase B (IC50 9.80 µM).

Conclusions:

• Benzofuran-pyrazole derivatives, especially compound 9, demonstrate significant potential as antimicrobial agents.
• Potent DNA gyrase B inhibition by compound 9 suggests a promising mechanism for combating resistant infections.
• Further development is warranted for clinical applications of these novel compounds.