Publikation: Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors : SAR and structural insights
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Datum
2011
Autor:innen
Grädler, Ulrich
Fuchß, Thomas
Ulrich, Wolf-Rüdiger
Boer, Rainer
Strub, Andreas
Hesslinger, Christian
Anézo, Céline
Zaliani, Andrea
Herausgeber:innen
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Published
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Bioorganic & Medicinal Chemistry Letters. 2011, 21(14), pp. 4228-4232. ISSN 0960-894X. eISSN 1464-3405. Available under: doi: 10.1016/j.bmcl.2011.05.073
Zusammenfassung
Inducible arginine oxidation and subsequent NO production by correspondent synthase (iNOS) are important cellular answers to proinflammatory signals. Prolonged NO production has been proved in higher organisms to cause stroke or septic shock. Several classes of potent NOS inhibitors have been reported, most of them targeting the arginine binding site of the oxygenase domain. Here we disclose the SAR and the rational design of potent and selective iNOS inhibitors which may be useful as anti-inflammatory drugs.
Zusammenfassung in einer weiteren Sprache
Fachgebiet (DDC)
570 Biowissenschaften, Biologie
Schlagwörter
Nitric oxide synthase, inflammation, crystal structure, structure-based design, selectivity, inhibitor
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GRÄDLER, Ulrich, Thomas FUCHSS, Wolf-Rüdiger ULRICH, Rainer BOER, Andreas STRUB, Christian HESSLINGER, Céline ANÉZO, Kay DIEDERICHS, Andrea ZALIANI, 2011. Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors : SAR and structural insights. In: Bioorganic & Medicinal Chemistry Letters. 2011, 21(14), pp. 4228-4232. ISSN 0960-894X. eISSN 1464-3405. Available under: doi: 10.1016/j.bmcl.2011.05.073BibTex
@article{Gradler2011-07-15Novel-19253,
year={2011},
doi={10.1016/j.bmcl.2011.05.073},
title={Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors : SAR and structural insights},
number={14},
volume={21},
issn={0960-894X},
journal={Bioorganic & Medicinal Chemistry Letters},
pages={4228--4232},
author={Grädler, Ulrich and Fuchß, Thomas and Ulrich, Wolf-Rüdiger and Boer, Rainer and Strub, Andreas and Hesslinger, Christian and Anézo, Céline and Diederichs, Kay and Zaliani, Andrea}
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<dcterms:abstract xml:lang="eng">Inducible arginine oxidation and subsequent NO production by correspondent synthase (iNOS) are important cellular answers to proinflammatory signals. Prolonged NO production has been proved in higher organisms to cause stroke or septic shock. Several classes of potent NOS inhibitors have been reported, most of them targeting the arginine binding site of the oxygenase domain. Here we disclose the SAR and the rational design of potent and selective iNOS inhibitors which may be useful as anti-inflammatory drugs.</dcterms:abstract>
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