Neuroactive steroids with perfluorobenzoyl group
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11130%2F12%3A8123" target="_blank" >RIV/00216208:11130/12:8123 - isvavai.cz</a>
Alternative codes found
RIV/67985823:_____/12:00380142 RIV/61388963:_____/12:00380142
Result on the web
<a href="http://dx.doi.org/10.1016/j.steroids.2012.07.004" target="_blank" >http://dx.doi.org/10.1016/j.steroids.2012.07.004</a>
DOI - Digital Object Identifier
—
Alternative languages
Result language
angličtina
Original language name
Neuroactive steroids with perfluorobenzoyl group
Original language description
During an initial study in searching for the alternative derivatives suitable for photolabeling of neuroactive steroids, perfluorobenzoates and perfluorobenzamides in position 17 of 5 beta-androstan-3 alpha-ol were synthesized from the corresponding 17-hydroxy and 17-amino derivatives. After transformation into glutamates or sulfates, 17 alpha-epimers had comparable inhibitory activity at NMDA receptors to the natural neurosteroid (20-oxo-5 beta-pregnan-3 beta-yl sulfate), however, were more potent (2-to 36-fold) than their 17 beta-substituted analogs. In one case, fluorine in position 4' of perfluorobenzoate group was substituted with azide and activity of the final glutamate was retained comparing with the corresponding perfluorobenzoate. The serieswas expanded with perfluorobenzoyl derivatives of pregnanolone: Perfluorobenzamide of glutamate and perfluorobenzoate of 11 alpha-hydroxy pregnanolone were prepared and tested. From nine tested compounds, four of them exhibit very good i
Czech name
—
Czech description
—
Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FB - Endocrinology, diabetology, metabolism, nutrition
OECD FORD branch
—
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2012
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Steroids
ISSN
0039-128X
e-ISSN
—
Volume of the periodical
77
Issue of the periodical within the volume
12
Country of publishing house
US - UNITED STATES
Number of pages
9
Pages from-to
1233-1241
UT code for WoS article
000310480800008
EID of the result in the Scopus database
—