Abstract：
:Thirty-four novel, diaryl ω-(isothiocyanato)alkylphosphonates with chlorine atom and methoxy, dimethoxy, methylsulfanyl, or methoxycarbonyl groups at ortho, meta, or para positions of the phenyl ring, and with an unbranched alkyl chain (n = 2-6) were designed and synthesized in a one-pot reaction in 11-76% yields. All isothiocyanates thus generated were evaluated for the first time for antibacterial activity on Pseudomonas aeruginosa and Staphylococcus aureus bacterial strains, and had satisfactory antibacterial activity in most cases. The highest activity, similar to that of reference gentamicin activity against S. aureus, was seen in compounds 9 and 13 (1.5 ± 0.1 and 2.5 ± 0.2 μM, respectively), whereas for P. aeruginosa more than half of tested compounds proved to be more effective than gentamicin. Additionally, selected isothiocyanates (9, 13, 18, and 23) were transformed in 52-73% yields into mercapturic acids 42-45, which also exhibited satisfactory antibacterial effect against S. aureus strain.
journal_name
Life Scijournal_title
Life sciencesauthors
Janczewski Ł,Burchacka E,Psurski M,Ciekot J,Gajda A,Gajda Tdoi
10.1016/j.lfs.2019.01.020subject
Has Abstractpub_date
2019-02-15 00:00:00pages
264-271eissn
0024-3205issn
1879-0631pii
S0024-3205(19)30030-Xjournal_volume
219pub_type
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