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Salicylanilide diethyl phosphates: Synthesis, antimicrobial activity and cytotoxicity
- 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.
- Subjects :
- Antifungal Agents
Cell Survival
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
Microbial Sensitivity Tests
Salicylanilides
Biochemistry
Microbiology
Mycobacterium tuberculosis
Structure-Activity Relationship
Minimum inhibitory concentration
chemistry.chemical_compound
Drug Discovery
Humans
Molecular Biology
Cell Proliferation
Mycobacterium kansasii
Bacteria
Dose-Response Relationship, Drug
Molecular Structure
biology
Chemistry
Organic Chemistry
Fungi
Hep G2 Cells
biology.organism_classification
Antimicrobial
Organophosphates
Anti-Bacterial Agents
Hep G2
Salicylanilide
Molecular Medicine
Drug Screening Assays, Antitumor
Mycobacterium
Subjects
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