Abstract
This article represents a mini-review dedicated to chalcone derivatives with antimycobacterial activity. Natural and synthetic chlacones are reviewed. General and specific schemes of synthesis of chalchone derivatives are presented. QSAR and docking studies of certain chalcones are analyzed in respect of their antimycobacterial activity and inhibition of Mycobacterium tuberculosis enzymes.
Highlights
Chalcones structurally represent open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α,β-unsaturated carbonyl system (1,3-diphenyl-2-propen-1-one)
The review has as its main purpose analysis and generalization of the data obtained so far on chalcone derivatives with activity against Mycobacterium tuberculosis
A group of naphthylchalcone derivatives have been studied for their inhibitory properties against M. tuberculosis protein tyrosine phosphatase A (MtbPtpA) [10,11]
Summary
Chalcones structurally represent open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α,β-unsaturated carbonyl system (1,3-diphenyl-2-propen-1-one). This way, Sivakumar et al [7] have synthesized 25 chalcone derivatives and performed QSAR studies of their antimycobacterial activity. According to their results introduction of -NMe2, -OMe, -SMe groups in different positions of the ring B led to the increase of anti-tuberculosis activity as compared to unsubstituted chalcone.
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