Design and synthesis of new steroid-derivatives with antibacterial activity on Salmonella typhi

In this study, the following estrogen derivatives were synthesized; oxazin-estradiol-3,17-diol (6), oxazine-estradiol-3,17-diylbis-2-chloroacetate (8), chloro-acetic acid-estradiol ester (9), 3,17-bis-(tert-butyl-dimethyl-silanyloxy)-estradiol-1,2-diamine (10) and 3,17-bis-(tert-butyl-dimethyl-silanyloxy)-estradiol-chloro-acetamide (11) using several strategies. The structure of compounds obtained was confirmed by elemental analysis, spectroscopy and spectrometry data. On the other hand, antibacterial activity of compounds synthesized was evaluated on Salmonella typhi with broth dilution methods to determine the minimal inhibitory concentration using gentamycin, ciprofloxacin and cefotaxime as controls. The results indicate that only the compounds 6, 9, 10 and 11 decrease the growth of Salmonella typhi. The methods used for synthesis of estrogen derivatives offers some advantages such as simple procedure, low cost and ease of workup. In addition, the antibacterial activity showed the compounds 6, 9, 10 and 11 depend on chemical structure in comparison with the controls involved. These estrogenic derivatives could be used as a therapeutic alternative for treatment of infectious diseases induced by Salmonella typhi.