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Xanthone: A Promising Antimycobacterial Scaffold

Author(s):

Tilal Elsaman, Malik Suliman Mohamed, Eyman Mohamed Eltayib, Abualgasim Elgaili Abdalla and Magdi Awadalla Mohamed*   Pages 1 - 22 ( 22 )

Abstract:


Background: Tuberculosis (TB) is one of the infectious diseases associated with high rate of morbidity and mortality and still remains one of the top-ten leading causes of human death in the world. Development of new anti-TB drugs is mandatory due to existence of latent infection as well as the expansion of the resistant Mycobacterium tuberculosis (MBT) strains. Xanthones encompass a wide range of structurally diverse bioactive compounds, obtained either naturally or through chemical synthesis. There is a growing body of literature that recognizes the antitubercular activity of xanthone derivatives.

Objective: The objective of this review is to highlight the main natural sources along with the critical design elements, structure-activity relationships (SARs), modes of action and pharmacokinetic profiles of xanthone-based anti-TB compounds.

Method: In the present review, the anti-TB activity of xanthones reported in the literature from 1972 to date is presented and discussed.

Results: Exploration of xanthone scaffold led to identification of several members of this class having superior activity against both sensitive and resistant MBT strains with distinctive mycobacterial membrane disrupting properties. However, studies regarding their modes of action, pharmacokinetic properties and safety are so limited.

Conclusion: Comprehendible data and information are afforded by this review and it would certainly provide scientists with new thoughts and means which will be conducive to design and develop new drugs with excellent anti-TB activity through exploration of xanthone scaffold.

Keywords:

Xanthones, mycobacterium tuberculosis, drug-resistant tuberculosis, structure-activity relationships (SARs), Membrane-targeting properties, Pharmacokinetic profiles.

Affiliation:

Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, Jouf University, Sakaka, Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka



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