摘要

Some [arylidenamino]-1,3,4-thiadiazino[6,5-b] indoles were synthesized starting from indole-2,3-dione, thiosemicarbazide and aromatic aldehydes with activating and deactivating groups. Inclusion complexes of these compounds were prepared with beta-cyclodextrin to increase their solubility and bioaccessibility. Thermodynamic properties like change in free energy, change in enthalpy, change in entropy and stability constant of the inclusion complexes were determined in order to elucidate whether the inclusion complex formation is thermodynamically allowed or not. The compounds and their inclusion complexes were screened against S. aureus and E. coli. It was found that the antibacterial activities of the compounds significantly increase after inclusion complex formation.

  • 出版日期2013