Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one
Disodium 2β,3α-dihydroxy-5α-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...
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2011
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| Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0039128X_v76_n10-11_p1160_Richmond http://hdl.handle.net/20.500.12110/paper_0039128X_v76_n10-11_p1160_Richmond |
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paper:paper_0039128X_v76_n10-11_p1160_Richmond2023-06-08T15:03:20Z Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one Maier, Marta Silvia Acetylcholinesterase activity Sulfated steroids Synthesis 2 beta,3 alpha dihydroxy 5 alpha cholestane disulfate acetylcholinesterase cholesterol cholesterol mesylate cholinesterase inhibitor disodium 2 beta,3 alpha dihydroxy 5 alpha cholestan 6 one disulfate n,n dimethylformamide oxide sulfur trioxide trimethylamine unclassified drug article drug activity drug sulfation drug synthesis enzyme activity enzyme inhibition IC 50 in vitro study Acetylcholinesterase Enzyme Activation Kinetics Magnetic Resonance Spectroscopy Steroids Disodium 2β,3α-dihydroxy-5α-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 2β,3α-dihydroxy- 5α-cholestane disulfate (10) and diols 7 and 9. Compounds 8 and 10 were active with IC50 values of 14.59 and 59.65 μM, respectively. Diols 7 and 9 showed no inhibitory activity (IC50 > 500 μM). © 2011 Elsevier Inc. All rights reserved. Fil:Maier, M.S. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. 2011 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0039128X_v76_n10-11_p1160_Richmond http://hdl.handle.net/20.500.12110/paper_0039128X_v76_n10-11_p1160_Richmond |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
Acetylcholinesterase activity Sulfated steroids Synthesis 2 beta,3 alpha dihydroxy 5 alpha cholestane disulfate acetylcholinesterase cholesterol cholesterol mesylate cholinesterase inhibitor disodium 2 beta,3 alpha dihydroxy 5 alpha cholestan 6 one disulfate n,n dimethylformamide oxide sulfur trioxide trimethylamine unclassified drug article drug activity drug sulfation drug synthesis enzyme activity enzyme inhibition IC 50 in vitro study Acetylcholinesterase Enzyme Activation Kinetics Magnetic Resonance Spectroscopy Steroids |
| spellingShingle |
Acetylcholinesterase activity Sulfated steroids Synthesis 2 beta,3 alpha dihydroxy 5 alpha cholestane disulfate acetylcholinesterase cholesterol cholesterol mesylate cholinesterase inhibitor disodium 2 beta,3 alpha dihydroxy 5 alpha cholestan 6 one disulfate n,n dimethylformamide oxide sulfur trioxide trimethylamine unclassified drug article drug activity drug sulfation drug synthesis enzyme activity enzyme inhibition IC 50 in vitro study Acetylcholinesterase Enzyme Activation Kinetics Magnetic Resonance Spectroscopy Steroids Maier, Marta Silvia Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one |
| topic_facet |
Acetylcholinesterase activity Sulfated steroids Synthesis 2 beta,3 alpha dihydroxy 5 alpha cholestane disulfate acetylcholinesterase cholesterol cholesterol mesylate cholinesterase inhibitor disodium 2 beta,3 alpha dihydroxy 5 alpha cholestan 6 one disulfate n,n dimethylformamide oxide sulfur trioxide trimethylamine unclassified drug article drug activity drug sulfation drug synthesis enzyme activity enzyme inhibition IC 50 in vitro study Acetylcholinesterase Enzyme Activation Kinetics Magnetic Resonance Spectroscopy Steroids |
| description |
Disodium 2β,3α-dihydroxy-5α-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 2β,3α-dihydroxy- 5α-cholestane disulfate (10) and diols 7 and 9. Compounds 8 and 10 were active with IC50 values of 14.59 and 59.65 μM, respectively. Diols 7 and 9 showed no inhibitory activity (IC50 > 500 μM). © 2011 Elsevier Inc. All rights reserved. |
| author |
Maier, Marta Silvia |
| author_facet |
Maier, Marta Silvia |
| author_sort |
Maier, Marta Silvia |
| title |
Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one |
| title_short |
Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one |
| title_full |
Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one |
| title_fullStr |
Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one |
| title_full_unstemmed |
Synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one |
| title_sort |
synthesis and acetylcholinesterase inhibitory activity of 2β,3α-disulfoxy-5α-cholestan-6-one |
| publishDate |
2011 |
| url |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0039128X_v76_n10-11_p1160_Richmond http://hdl.handle.net/20.500.12110/paper_0039128X_v76_n10-11_p1160_Richmond |
| work_keys_str_mv |
AT maiermartasilvia synthesisandacetylcholinesteraseinhibitoryactivityof2b3adisulfoxy5acholestan6one |
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