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Statements

Subject Item
n2:RIV%2F00216208%3A11110%2F13%3A10190173%21RIV14-MSM-11110___
rdf:type
n7:Vysledek skos:Concept
rdfs:seeAlso
http://dx.doi.org/10.1016/j.bmc.2012.12.019
dcterms: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. 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.
dcterms:title
Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase
skos:prefLabel
Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase
skos:notation
RIV/00216208:11110/13:10190173!RIV14-MSM-11110___
n7:predkladatel
n15:orjk%3A11110
n3:aktivita
n16:Z
n3:aktivity
Z(MSM0021620849)
n3:cisloPeriodika
5
n3:dodaniDat
n14:2014
n3:domaciTvurceVysledku
n17:4688678
n3:druhVysledku
n9:J
n3:duvernostUdaju
n13:S
n3:entitaPredkladatele
n20:predkladatel
n3:idSjednocenehoVysledku
67620
n3:idVysledku
RIV/00216208:11110/13:10190173
n3:jazykVysledku
n18:eng
n3:klicovaSlova
synthase; oxide; nitric; neuronal; inhibitors; methyl-containing; Cyclopropyl-
n3:klicoveSlovo
n10:methyl-containing n10:synthase n10:Cyclopropyl- n10:inhibitors n10:nitric n10:neuronal n10:oxide
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[1E2629C10AD1]
n3:nazevZdroje
Bioorganic and Medicinal Chemistry
n3:obor
n21:CE
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
11
n3:rokUplatneniVysledku
n14:2013
n3:svazekPeriodika
21
n3:tvurceVysledku
Ji, Haitao Roman, Linda J. Mataka, Jan Silverman, Richard B. Xue, Fengtian Poulos, Thomas L. Martásek, Pavel Labby, Kristin Jansen Kraus, James M., II Delker, Silvia L. Li, Huiying
n3:wos
000314689200033
n3:zamer
n8:MSM0021620849
s:issn
0968-0896
s:numberOfPages
11
n5:doi
10.1016/j.bmc.2012.12.019
n19:organizacniJednotka
11110