Xanthone: A Promising Antimycobacterial Scaffold

Area of Science:

• Medicinal Chemistry
• Pharmacology
• Microbiology

Background:

• Tuberculosis (TB) remains a leading cause of death globally, necessitating new drug development due to latent infections and resistant Mycobacterium tuberculosis (MBT) strains.
• Xanthones, a diverse class of natural and synthetic compounds, are recognized for their potential antitubercular activity.

Purpose of the Study:

• To review natural sources, design elements, structure-activity relationships (SARs), modes of action, and pharmacokinetics of xanthone-based anti-TB compounds.
• To consolidate existing knowledge on xanthones for the development of novel anti-TB therapeutics.

Main Methods:

• Comprehensive literature review of anti-TB xanthone research from 1972 to the present.
• Analysis of reported antitubercular activity, SARs, and mechanisms of action.

Main Results:

• Xanthone scaffolds have yielded compounds with significant activity against both sensitive and resistant MBT strains.
• Identified compounds exhibit distinct properties, including mycobacterial membrane disruption.
• Limited data exists on the detailed modes of action, pharmacokinetics, and safety profiles of these xanthone derivatives.

Conclusions:

• This review provides valuable data for scientists to design and develop novel anti-TB drugs.
• Exploration of the xanthone scaffold offers a promising avenue for creating effective antitubercular agents.