title: New derivatives of salicylamides: Preparation and antimicrobial activity against various bacterial species.
abstract: 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.
authors.affiliation: Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentská 573, 532 10 Pardubice, Czech Republic.
authors.forename: Karel
authors.initials: K
authors.lastname: Pauk
authors.forename: Iveta
authors.initials: I
authors.lastname: Zadražilová
authors.forename: Aleš
authors.initials: A
authors.lastname: Imramovský
authors.forename: Jarmila
authors.initials: J
authors.lastname: Vinšová
authors.forename: Michaela
authors.initials: M
authors.lastname: Pokorná
authors.forename: Martina
authors.initials: M
authors.lastname: Masaříková
authors.forename: Alois
authors.initials: A
authors.lastname: Cížek
authors.forename: Josef
authors.initials: J
authors.lastname: Jampílek
mesh_terms: D000667:Ampicillin / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002939:Ciprofloxacin / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D012457:Salicylamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D012457:Salicylamides; D002939:Ciprofloxacin; D000667:Ampicillin
keywords: Antibacterial; Antimycobacterial; Salicylamide derivatives