New derivatives of salicylamides: Preparation and antimicrobial activity against various bacterial species
| Autor: | Josef Jampilek, Alois Čížek, Aleš Imramovský, Martina Masaříková, Karel Pauk, Iveta Zadražilová, Jarmila Vinšová, Michaela Pokorná |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
medicine.drug_class
Stereochemistry Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Gram-Positive Bacteria Antimycobacterial Biochemistry Structure-Activity Relationship Anti-Infective Agents Ciprofloxacin Ampicillin Gram-Negative Bacteria Salicylamides Drug Discovery medicine Organic chemistry Molecular Biology Chemistry Organic Chemistry Salicylanilides Antimicrobial Molecular Medicine medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry. 21:6574-6581 |
| ISSN: | 0968-0896 |
| Popis: | Three series of salicylanilides, esters of N-phenylsalicylamides and 2-hydroxy-N-[1-(2-hydroxyphenylamino)-1-oxoalkan-2-yl]benzamides, in total thirty target compounds were synthesized and characterized. The compounds were evaluated against seven bacterial and three mycobacterial strains. The antimicrobial activities of some compounds were comparable or higher than the standards ampicillin, ciprofloxacin or isoniazid. Derivatives 3f demonstrated high biological activity against Staphylococcus aureus (⩽0.03μmol/L), Mycobacterium marinum (⩽0.40μmol/L) and Mycobacterium kansasii (1.58μmol/L), 3g shows activity against Clostridium perfringens (⩽0.03μmol/L) and Bacillus cereus (0.09μmol/L), 3h against Pasteurella multocida (⩽0.03μmol/L) and M. kansasii (⩽0.43μmol/L), 3i against methicillin-resistant S. aureus and B. cereus (⩽0.03μmol/L). The structure-activity relationships are discussed for all the compounds. |
| Databáze: | OpenAIRE |
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