Abstract
A series of 27 salicylanilide diethyl phosphates was prepared as a part of our on-going search for new antimicrobial active drugs. All compounds exhibited in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium strains, with minimum inhibitory concentration (MIC) values of 0.5-62.5μmol/L. Selected salicylanilide diethyl phosphates also inhibit multidrug-resistant tuberculous strains at the concentration of 1μmol/L. Salicylanilide diethyl phosphates also exhibited mostly the activity against Gram-positive bacteria (MICs ≥1.95μmol/L), whereas their antifungal activity is significantly lower. The IC50 values for Hep G2 cells were within the range of 1.56-33.82μmol/L, but there is no direct correlation with MICs for mycobacteria.
Keywords:
Cytotoxicity; Diethyl phosphate; In vitro antimicrobial activity; In vitro antimycobacterial activity; Salicylanilide.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Antifungal Agents / chemical synthesis
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology*
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Bacteria / drug effects*
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Fungi / drug effects*
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Hep G2 Cells
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Humans
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Microbial Sensitivity Tests
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Molecular Structure
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Organophosphates / chemical synthesis
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Organophosphates / chemistry
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Organophosphates / pharmacology*
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Salicylanilides / chemical synthesis
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Salicylanilides / chemistry
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Salicylanilides / pharmacology*
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Antifungal Agents
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Antineoplastic Agents
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Organophosphates
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Salicylanilides