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Xanthone: A Promising Antimycobacterial Scaffold
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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.
The development of new anti-TB drugs is mandatory due to the 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.
Methods:
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 the 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 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.
Bentham Science Publishers Ltd.
Title: Xanthone: A Promising Antimycobacterial Scaffold
Description:
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.
The development of new anti-TB drugs is mandatory due to the 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.
Methods:
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 the 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 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.
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