TB is one of the major infectious diseases caused by Mycobacterium tuberculosis (M.TB)
with millions of people dying every year. Emergence of new cases, increased incidence of multi drug
resistant strains of M.TB and the adverse effects of first and second line antitubercular drugs have led to
renewed interest in natural products with the hope of discovering new antitubercular leads. Coumarins
and chalcones are plant derived secondary metabolites with potentially exploitable activities against
M.TB. To pave way for future antitubercular research, there is an urgent need to collect latest information
on these promising moieties. The objective of this review is to focus on the newer and important
coumarin and chalcone derivatives having potent antitubercular activity. General scheme of synthesis of
coumarins and chalcones is presented. This review enlightens the landscape of the discovery and development
of chalcones and coumarin based antitubercular drugs with an emphasis on Structure- Activity
Relationship (SAR) and inhibition of some their specific molecular targets. We hope that this review
paper would provide new opportunities for researchers to design future generation novel and potent
coumarin and chalcone based antitubercular drugs with higher activity and lesser toxicity.
Keywords: Antitubercular activity, Mycobacterium tuberculosis, QSAR Studies, Molecular targets, Chalcones, Coumarins.
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