N-substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidines - antibacterial, cytotoxic activities and some structure-activity relationships
Beata Żołnowska , Jarosław Sławiński , Aleksandra Grzonek , Anna Kędzia , Ewa Kwapisz , Anna Kawiak
AbstractA 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 Enterococcus faecalis . It was found that Parvimonas micra , Finegoldia magna , Peptostrepto - coccus anaerobius , Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.
|Journal series||Polish Journal of Microbiology, ISSN 1733-1331, (A 15 pkt)|
|Publication size in sheets||0.5|
|Keywords in English||2-mercaptobenzenesulfonamide, antibacterial activity, polar surface area, sulfonylguanidine, theoretical calculations|
|License||Journal (articles only); published final; ; with publication|
|Score|| = 15.0, ArticleFromJournal|
= 15.0, ArticleFromJournal
|Publication indicators||: 2015 = 0.75 (2) - 2015=0.993 (5)|
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