Novel steroidal oestrogens, that incorporate some of the structural motifs of non-steroidal antioestrogens, were synthesised and tested for their actions on the BK channel. These novel compounds were first checked for purity and structure using, where appropriate, 1H NMR, 13C NMR, IR spectroscopy, mass spectroscopy, thin layer chromatography, melting point analysis, elemental analysis and X-ray crystallography. Using Oestrone as the starting compound, the following five novel compounds were synthesised; DME-Oestrone, Quat-DME-Oestrone, DME-Oestradiol, Quat-DME-Oestradiol and Oestrone-Oxime. Two of the derivatives, Quat-DME-Oestrone and Quat-DME-Oestradiol, incorporated a quaternary ammonium side-chain making them membrane impermeable.
|Date of Award
|Marcus Allen (Supervisor)