Abstract
Salicylanilides have been a subject of interest in medicinal chemistry as a group with a wide range of biological activities. The antibacterial (including antimycobacterial) and antifungal activities have come to be viewed as very significant. The synthesis of new prodrugs to counter a number of problematic properties of salicylanilides is a current trend. This article brings together the known basic facts about these prodrugs, particularly about the different mechanisms of the antimicrobial action of salicylanilides, including salicylanilide toxicity and undesired effects. The largest part of this group consists of antimicrobial salicylanilide esters with different organic acids, e.g. acetates, carbamates, esters with N-protected amino acids, and mutual antibacterial compounds with known antibacterial agents (β-lactames and linezolid), with the activity and structure-activity relationships of these compounds being of particular interest. This review summarizes the activity of salicylanilides as potential virulence inhibitors attributable to a blockade of the type III secretion pathway. Many salicylanilide ester derivatives have been demonstrated an effective and promising treatment against pathogenic fungi and bacteria (especially against Gram-positive, tuberculous and atypical mycobacterial strains), including strains such as methicillinresistant Staphylococcus aureus and isoniazid-resistant mycobacteria which are resistant to one or more clinically used drugs.
Keywords: Prodrug, salicylanilide, salicylanilide ester, antibacterial activity, antimycobacterial activity, antifungal activity, glucose oxidation, glucose fermentation, photophosphorylation, antibiotics
Current Pharmaceutical Design
Title: Salicylanilide Ester Prodrugs as Potential Antimicrobial Agents - a Review
Volume: 17 Issue: 32
Author(s): Martin Kratky and Jarmila Vinsova
Affiliation:
Keywords: Prodrug, salicylanilide, salicylanilide ester, antibacterial activity, antimycobacterial activity, antifungal activity, glucose oxidation, glucose fermentation, photophosphorylation, antibiotics
Abstract: Salicylanilides have been a subject of interest in medicinal chemistry as a group with a wide range of biological activities. The antibacterial (including antimycobacterial) and antifungal activities have come to be viewed as very significant. The synthesis of new prodrugs to counter a number of problematic properties of salicylanilides is a current trend. This article brings together the known basic facts about these prodrugs, particularly about the different mechanisms of the antimicrobial action of salicylanilides, including salicylanilide toxicity and undesired effects. The largest part of this group consists of antimicrobial salicylanilide esters with different organic acids, e.g. acetates, carbamates, esters with N-protected amino acids, and mutual antibacterial compounds with known antibacterial agents (β-lactames and linezolid), with the activity and structure-activity relationships of these compounds being of particular interest. This review summarizes the activity of salicylanilides as potential virulence inhibitors attributable to a blockade of the type III secretion pathway. Many salicylanilide ester derivatives have been demonstrated an effective and promising treatment against pathogenic fungi and bacteria (especially against Gram-positive, tuberculous and atypical mycobacterial strains), including strains such as methicillinresistant Staphylococcus aureus and isoniazid-resistant mycobacteria which are resistant to one or more clinically used drugs.
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Cite this article as:
Kratky Martin and Vinsova Jarmila, Salicylanilide Ester Prodrugs as Potential Antimicrobial Agents - a Review, Current Pharmaceutical Design 2011; 17 (32) . https://dx.doi.org/10.2174/138161211798194521
DOI https://dx.doi.org/10.2174/138161211798194521 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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