MURRAY Ana paula
Synthesis and acetylcholinesterase inhibitory activity of 2beta,3alfa-disulfoxy-5alfa-cholestan-6-one
RICHMOND, VICTORIA; GARRIDO SANTOS, GUSTAVO; ANA PAULA MURRAY; MAIER, MARTA SILVIA
ELSEVIER SCIENCE INC
Año: 2011 vol. 76 p. 1160 - 1165
Disodium 2beta,3alfa-dihydroxy-5alfa-cholestan-6-one disulfate (8) has been synthesized using cholesterol (1) as starting material. Sulfation was performed using trimethylamine-sulfur trioxide complex in dimethylformamide as the sulfating agent. The acetylcholinesterase inhibitory activity of compound 8 was evaluated and compared to that of disodium 2b,3a-dihydroxy-5a-cholestane disulfate (10) and diols 7 and 9. Compounds 8 and 10 were active with IC50 values of 14.59 and 59.65 microM, respectively. Diols 7 and 9 showed no inhibitory activity (IC50 > 500 microM).