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

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About: Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase Goto Sponge NotDistinct Permalink

An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://dx.doi.org/10.1016/j.bmc.2012.12.019
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. (en)
Title	Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase (en)
skos:prefLabel	Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase (en)
skos:notation	RIV/00216208:11110/13:10190173!RIV14-MSM-11110___
http://linked.open...avai/predkladatel	1. lékařská fakulta
http://linked.open...avai/riv/aktivita	Z
http://linked.open...avai/riv/aktivity	Z(MSM0021620849)
http://linked.open...iv/cisloPeriodika	5
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Martásek, Pavel
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Univerzita Karlova v Praze / 1. lékařská fakulta
http://linked.open...dnocenehoVysledku	67620
http://linked.open...ai/riv/idVysledku	RIV/00216208:11110/13:10190173
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	synthase; oxide; nitric; neuronal; inhibitors; methyl-containing; Cyclopropyl- (en)
http://linked.open.../riv/klicoveSlovo	Cyclopropyl- methyl-containing nitric synthase inhibitors oxide neuronal
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[1E2629C10AD1]
http://linked.open...i/riv/nazevZdroje	Bioorganic and Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	1 (xsd:int)
http://linked.open...cetTvurcuVysledku	11 (xsd:int)
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	21
http://linked.open...iv/tvurceVysledku	Martásek, Pavel Li, Huiying Poulos, Thomas L. Roman, Linda J. Silverman, Richard B. Delker, Silvia L. Ji, Haitao Kraus, James M., II Labby, Kristin Jansen Mataka, Jan Xue, Fengtian
http://linked.open...ain/vavai/riv/wos	000314689200033
http://linked.open...n/vavai/riv/zamer	Neuropsychiatrické aspekty neurodegenerativních onemocnění
issn	0968-0896
number of pages	11 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.bmc.2012.12.019
http://localhost/t...ganizacniJednotka	11110

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