Synthesis and in vitro antibacterial activity of 5-Halogenomethylsulfonyl- benzimidazole and benzotriazole derivatives
Zbigniew Ochal , Maria Bretner , Renata Wilinowska , Stefan Tyski
AbstractA series of 5-halogenomethylsulfonylbenzimidazole and benzotriazole derivatives was synthesized as potential antibacterial agents. A new method of synthesis of benzimidazoles was developed. The antimicrobial activities of these compounds were tested against a series of reference and clinical strains. The reference strains include Gram-positive bacteria (S. aureus, S. epidermidis, B. subtilis, B. cereus, E. hirae, M. luteus) and Gram-negative rods (E. coli, P. vulgaris, P. aeruginosa, B. bronchiseptica). The clinical strains include six methicillin-resistant (MRSA) and two methicillin-sensitive (MSSA) S. aureus strains, one methicillin-resistant S. epidermidis, three E. faecalis and two E. faecium strains. Compound with trifluoromethyl- substituent at C-2 position (4) displayed significant antibacterial activities comparable with nitrofurantoin against four strains, and higher against Micrococcus luteus. MIC values for clinical Staphylococci strains (MRSA) were 12.5-25 μg/mL; for Enterococcus strains these values were 50-100 μg/mL. MIC values for reference and clinical strains of Staphylococcus and Enterococcus group were similar, respectively.
|Journal series||Medicinal Chemistry, ISSN 1573-4064, [1875-6638 ]|
|Publication size in sheets||0.3|
|Keywords in English||5-Halogenomethylsulfonylbenzimidazole and benzotriazole derivatives, Amberlyst 15, Antibacterial activity, MRSA, MSSA, Nitrofurantoin|
|Score|| = 15.0, 02-02-2020, ArticleFromJournal|
= 20.0, 02-02-2020, ArticleFromJournal
|Publication indicators||= 10; = 8; : 2014 = 0.652; : 2013 = 1.387 (2) - 2013=1.379 (5)|
|Citation count*||1 (2014-08-16)|
* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or Perish system.