Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11110%2F13%3A10190173" target="_blank" >RIV/00216208:11110/13:10190173 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1016/j.bmc.2012.12.019" target="_blank" >http://dx.doi.org/10.1016/j.bmc.2012.12.019</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmc.2012.12.019" target="_blank" >10.1016/j.bmc.2012.12.019</a>

Result language
angličtina
Original language name
Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase
Original language description
Inhibitors of neuronal nitric oxide synthase have been proposed as therapeutics for the treatment of different types of neurological disorders. On the basis of a cis-3,4-pyrrolidine scaffold, a series of trans-cyclopropyl- and methyl-containing nNOS inhibitors have been synthesized. The insertion of a rigid electron-withdrawing cyclopropyl ring decreases the basicity of the adjacent amino group, which resulted in decreased inhibitory activity of these inhibitors compared to the parent compound. Nonetheless, three of them exhibited double-digit nanomolar inhibition with high nNOS selectivity on the basis of in vitro enzyme assays. Crystal structures of nNOS and eNOS with these inhibitors bound provide a basis for detailed structure-activity relationship(SAR) studies. The conclusions from these studies will be used as a guide in the future development of selective NOS inhibitors.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CE - Biochemistry
OECD FORD branch
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Publication year
2013
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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