Chalcone scaffolds as anti-infective agents: Structural and molecular target perspectives

In recent years, widespread outbreak of numerous infectious diseases across the globe has created havoc among the population. Particularly, the inhabitants of tropical and sub-tropical regions are mainly affected by these pathogens. Several natural and (semi) synthetic chalcones deserve the credit o...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2015-08, Vol.101, p.496-524
Main Authors: Mahapatra, Debarshi Kar, Bharti, Sanjay Kumar, Asati, Vivek
Format: Article
Language:English
Subjects:
Animals
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacology
Anti-malarial
Anti-parasitic
Chalcone
Chalcone - chemical synthesis
Chalcone - chemistry
Chalcone - pharmacology
Drug Design
Enzymes - metabolism
Humans
Mechanism of actions
Molecular Structure
Molecular targets
Structure activity relationships
Structure-Activity Relationship
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Summary:In recent years, widespread outbreak of numerous infectious diseases across the globe has created havoc among the population. Particularly, the inhabitants of tropical and sub-tropical regions are mainly affected by these pathogens. Several natural and (semi) synthetic chalcones deserve the credit of being potential anti-infective candidates that inhibit various parasitic, malarial, bacterial, viral, and fungal targets like cruzain-1/2, trypanopain-Tb, trans-sialidase, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), fumarate reductase, falcipain-1/2, β-hematin, topoisomerase-II, plasmepsin-II, lactate dehydrogenase, protein kinases (Pfmrk and PfPK5), and sorbitol-induced hemolysis, DEN-1 NS3, H1N1, HIV (Integrase/Protease), protein tyrosine phosphatase A/B (Ptp-A/B), FtsZ, FAS-II, lactate/isocitrate dehydrogenase, NorA efflux pump, DNA gyrase, fatty acid synthase, chitin synthase, and β-(1,3)-glucan synthase. In this review, a comprehensive study (from Jan. 1982 to May 2015) of the structural features of anti-infective chalcones, their mechanism of actions (MOAs) and structure activity relationships (SARs) have been highlighted. With the knowledge of molecular targets, structural insights and SARs, this review may be helpful for (medicinal) chemists to design more potent, safe, selective and cost effective anti-infective agents. In this review, a comprehensive study of anti-infective chalcones, their molecular targets, Structure Activity Relationships (SARs) and Mechanism of Actions (MOAs) have been described. [Display omitted] •Current status of infectious diseases across the globe.•Synthetic routes to benzylideneacetophenone (chalcone) scaffold.•Chalcones and their molecular targets for anti-infective activities.•Structures and SARs of various anti-infective chalcones.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2015.06.052