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

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 Enterococcus faecalis . It was found that Parvimonas micra , Finegoldia magna , Peptostrepto - coccus anaerobius , Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.
Author Beata Żołnowska
Beata Żołnowska,,
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, Jarosław Sławiński
Jarosław Sławiński,,
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, Aleksandra Grzonek
Aleksandra Grzonek,,
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, Anna Kędzia
Anna Kędzia,,
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, Ewa Kwapisz
Ewa Kwapisz,,
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, Anna Kawiak (IFB / IB / DBiotech) - [Medical Uniwersity of Gdańsk (GUMed)]
Anna Kawiak,,
- Department of Biotechnology
- Gdański Uniwersytet Medyczny
Journal seriesPolish Journal of Microbiology, ISSN 1733-1331, (A 15 pkt)
Issue year2015
Vol64
No3
Pages299-305
Publication size in sheets0.5
Keywords in English2-mercaptobenzenesulfonamide, antibacterial activity, polar surface area, sulfonylguanidine, theoretical calculations
URL http://www.pjm.microbiology.pl/archive/vol6432015299.pdf
Languageen angielski
LicenseJournal (articles only); published final; Other open licence; with publication
Score (nominal)15
ScoreMinisterial score = 15.0, 20-12-2017, ArticleFromJournal
Ministerial score (2013-2016) = 15.0, 20-12-2017, ArticleFromJournal
Publication indicators WoS Impact Factor: 2015 = 0.75 (2) - 2015=0.993 (5)
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