| The study introduces different organosilicon derivatives incorporating sulfanyltetrazole ring for biological applications.
Initially, the sulfanyltetrazole derivatives and halo-analogues (Br, I) were synthesized. Later, selective reaction of
tris(trimethylsilyl)methyllithium (TsiLi) in the presence (−46 and 0 °C) and absence (room temperature) of CS2
with
halo-sulfanyltetrazole derivatives yielded new multifunctional sulfanyltetrazole regioisomers with SH, C = S, ethynylthio
and SiMe3
groups, respectively. All the synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR spectra
and elemental analysis data. The compounds were screened for their antibacterial activities against clinically important
gram-positive and gram-negative bacteria using the spectrophotometric microdilution method. The preliminary screening
indicated that the organosilicon derivatives incorporating SH and C = S (mercapto-silyl-thiones) and silyl-thioalkynes have
antibacterial activities, whereas no antibacterial activity was observed on compounds containing (
Me3Si)3C groups. Of the
synthesized compounds, compound 5d showed the best activity against all the tested organisms (3.91–31.25 μg/mL). |