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Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity.
Vinsová, Jarmila; Kozic, Ján; Krátký, Martin; Stolaríková, Jirina; Mandíková, Jana; Trejtnar, Frantisek; Buchta, Vladimír.
Afiliação
  • Vinsová J; Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic. Electronic address: vinsova@faf.cuni.cz.
  • Kozic J; Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
  • Krátký M; Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
  • Stolaríková J; Laboratory for Mycobacterial Diagnostics and Tuberculosis, Regional Institute of Public Health in Ostrava, Partyzánské námestí 7, 702 00 Ostrava, Czech Republic.
  • Mandíková J; Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
  • Trejtnar F; Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
  • Buchta V; Department of Clinical Microbiology, Faculty of Medicine and University Hospital, Charles University, Sokolská 581, 500 12 Hradec Králové, Czech Republic; Department of Biological and Medical Sciences, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Bioorg Med Chem ; 22(2): 728-37, 2014 Jan 15.
Article em En | MEDLINE | ID: mdl-24369840
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Organofosfatos / Salicilanilidas / Bactérias / Fungos / Antibacterianos / Antifúngicos / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Organofosfatos / Salicilanilidas / Bactérias / Fungos / Antibacterianos / Antifúngicos / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article