Biphenyl as a Privileged Structure in Medicinal Chemistry: Advances in Anti-Infective Drug Discovery

Area of Science:

• Medicinal Chemistry
• Drug Discovery
• Pharmacology

Background:

• The rise of resistant fungal and viral strains presents a significant challenge in discovering novel anti-infective agents.
• The biphenyl subunit is recognized as a versatile privileged structure for drug design, enabling interactions with various protein targets.
• Biphenyl derivatives have shown potential in addressing the need for new anti-infective therapeutics.

Purpose of the Study:

• To review the pharmacological potential of biphenyl-based compounds as anti-infective agents.
• To analyze recent literature and rational design strategies for biphenyl derivatives in anti-infective drug development.
• To explore structure-activity relationships and optimization techniques for biphenyl-based anti-infectives.

Main Methods:

• Comprehensive literature analysis of biphenyl derivatives for anti-infective applications.
• Examination of rational design strategies, including structure-activity relationships and molecular docking.
• Evaluation of structural optimizations to improve pharmacodynamics and pharmacokinetics.

Main Results:

• Biphenyl moieties incorporated into compounds yield potent antifungal and antiviral activities.
• Optimized biphenyl derivatives demonstrate strong inhibition against resistant Candida strains and key viral targets like HIV-1 reverse transcriptase and protease.
• Strategic modifications improved metabolic stability and reduced cytotoxicity.

Conclusions:

• Biphenyl is a robust and adaptable scaffold for developing effective anti-infective agents.
• Rational structural optimization of biphenyl derivatives offers a viable strategy to overcome drug resistance.
• This approach facilitates the development of metabolically stable anti-infective therapeutics.