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Statements

Subject Item
n2:RIV%2F00064165%3A_____%2F10%3A7010%21RIV11-MZ0-00064165
rdf:type
skos:Concept n16:Vysledek
dcterms:description
Recently, a series of potent and selective neuronal nitric oxide synthase inhibitors containing two basic nitrogen atoms was reported (Ji, H.; Stanton, B. Z.; Igarashi, J.; Li, H.; Martasek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. J. Am. Chem. Soc. 2008, 130, 3900-3914). In an effort to improve their bioavailability, three compounds (2a-c) were designed with electron-withdrawing groups near one of the basic nitrogen atoms to lower its pK(a). Inhibition studies with these compounds showed that two of them not only retained most of the potency and selectivity of the best analogue of the earlier series, but also showed improved membrane permeability based on data from a cell-based assay. (C) 2009 Elsevier Ltd. All rights reserved. Recently, a series of potent and selective neuronal nitric oxide synthase inhibitors containing two basic nitrogen atoms was reported (Ji, H.; Stanton, B. Z.; Igarashi, J.; Li, H.; Martasek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. J. Am. Chem. Soc. 2008, 130, 3900-3914). In an effort to improve their bioavailability, three compounds (2a-c) were designed with electron-withdrawing groups near one of the basic nitrogen atoms to lower its pK(a). Inhibition studies with these compounds showed that two of them not only retained most of the potency and selectivity of the best analogue of the earlier series, but also showed improved membrane permeability based on data from a cell-based assay. (C) 2009 Elsevier Ltd. All rights reserved.
dcterms:title
Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability
skos:prefLabel
Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability
skos:notation
RIV/00064165:_____/10:7010!RIV11-MZ0-00064165
n3:aktivita
n8:Z n8:I n8:P
n3:aktivity
I, P(1M0520), Z(MSM0021620806)
n3:cisloPeriodika
2
n3:dodaniDat
n13:2011
n3:domaciTvurceVysledku
n14:4688678
n3:druhVysledku
n12:J
n3:duvernostUdaju
n11:S
n3:entitaPredkladatele
n17:predkladatel
n3:idSjednocenehoVysledku
280459
n3:idVysledku
RIV/00064165:_____/10:7010
n3:jazykVysledku
n18:eng
n3:klicovaSlova
Neuronal nitric oxide synthase; Selective inhibitors; Increased membrane permeability; pK(a); messenger-rna; disease
n3:klicoveSlovo
n10:messenger-rna n10:disease n10:Neuronal%20nitric%20oxide%20synthase n10:pK%28a%29 n10:Selective%20inhibitors n10:Increased%20membrane%20permeability
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[C1142DF450DB]
n3:nazevZdroje
Bioorganic & medicinal chemistry letters
n3:obor
n4:CE
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
6
n3:projekt
n15:1M0520
n3:rokUplatneniVysledku
n13:2010
n3:svazekPeriodika
20
n3:tvurceVysledku
Fang, JG Silverman, RB Roman, LJ Martásek, Pavel Xue, FT Lewis, WW
n3:wos
000272936000025
n3:zamer
n5:MSM0021620806
s:issn
0960-894X
s:numberOfPages
4