title: N-Substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidines--Antibacterial, Cytotoxic Activities and Some Structure-Activity Relationships.
abstract: A series of N-substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidine derivatives bearing sulfonamide moiety have been screened in vitro for antibacterial activity against isolates from patients with infections of oral cavity, respiratory tract and intestinal tract. The majority of compounds exhibited good antibacterial potency. 1-[4-Chloro-5-methyl-2-(4-trifluoromethylbenzylthio)benzenesulfonyl]-3-(3-sulfamoylphenyl)guanidine (13) showed very strong activity, with MIC ≤ 6.2 μg/ml against eleven bacteria strains belonged to Gram-positive anaerobes and aerobes. Furthermore, compound 13 exhibited promising activity toward highly resistant microorganisms such as methicillin-resistant Staphylococcus aureus and Enterococcusfaecalis. It was found that Parvimonas micra, Finegoldia magna, Peptostreptococcus anaerobius, Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.
authors.forename: Beata
authors.initials: B
authors.lastname: Zołnowska
authors.forename: Jarosław
authors.initials: J
authors.lastname: Sławiński
authors.forename: Aleksandra
authors.initials: A
authors.lastname: Grzonek
authors.forename: Anna
authors.initials: A
authors.lastname: Kędzia
authors.forename: Ewa
authors.initials: E
authors.lastname: Kwapisz
authors.forename: Anna
authors.initials: A
authors.lastname: Kawiak
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy / Q000382:microbiology; D006146:Guanidines / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D006146:Guanidines