Preparation, In Vitro Screening and Molecular Modelling of Monoquaternary Compounds Related to the Selective Acetylcholinesterase Inhibitor BW284c51
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F15%3A50003043" target="_blank" >RIV/62690094:18470/15:50003043 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/15:43875335 RIV/00179906:_____/15:10292633
Result on the web
<a href="http://benthamscience.com/journal/abstracts.php?journalID=mc&articleID=121875" target="_blank" >http://benthamscience.com/journal/abstracts.php?journalID=mc&articleID=121875</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.2174/1573406410666140428153110" target="_blank" >10.2174/1573406410666140428153110</a>
Alternative languages
Result language
angličtina
Original language name
Preparation, In Vitro Screening and Molecular Modelling of Monoquaternary Compounds Related to the Selective Acetylcholinesterase Inhibitor BW284c51
Original language description
This paper describes preparation and in vitro evaluation of 19 compounds related to the selective experimental cholinesterase inhibitor BW284c51. The novel compounds were prepared as fragments of parent molecule BW284c51 and evaluated on the model of human recombinant acetylcholinesterase and human plasmatic butyrylcholinesterase. The IC50 values of the prepared compounds were compared to the parent molecule BW284c51. None of the compounds was superior to the parent drug, but two BW284c51 fragments showed promising hAChE inhibition in M scale and improved selectivity. These two fragments were further subjected to the molecular modelling study and their enzyme interactions were rationalized. The structure-activity relationship of the prepared series wasstated.
Czech name
—
Czech description
—
Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
—
Result continuities
Project
—
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Medicinal chemistry
ISSN
1573-4064
e-ISSN
—
Volume of the periodical
11
Issue of the periodical within the volume
1
Country of publishing house
AE - UNITED ARAB EMIRATES
Number of pages
9
Pages from-to
21-29
UT code for WoS article
000349330100004
EID of the result in the Scopus database
—