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Salicylanilide diethyl phosphates: Synthesis, antimicrobial activity and cytotoxicity

Authors :
Ján Kozic
Jana Mandíková
František Trejtnar
Vladimír Buchta
Jiřina Stolaříková
Martin Krátký
Jarmila Vinšová
Source :
Bioorganic & Medicinal Chemistry. 22:728-737
Publication Year :
2014
Publisher :
Elsevier BV, 2014.

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.

Details

ISSN :
09680896
Volume :
22
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry
Accession number :
edsair.doi.dedup.....37c80d8485e00e8288890b2b27f38b0b
Full Text :
https://doi.org/10.1016/j.bmc.2013.12.016