Výsledky vyhledávání - "Nabil B. Ghazal"

2,3,4,5-Tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT2C agonists

Autor: Robert B McCall, Michael D. Ennis, Nabil B Ghazal, Deborah K Hyslop, Lawrence W Fitzgerald, Dac M. Dinh, Nanette F. Nichols, Michelle L Kagey, Christopher S Knauer, Robert L Hoffman, Chris L Chio, Rebecca M. Olson, Christopher L. Haber, Kjell A. Svensson, Jeffery E Campbell

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:2369-2372

The design and synthesis of the novel 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-a]indole 5 is described. This azepinoindole has excellent affinity for 5-HT(2C) (K(i) 4.8 nM) and modest selectivity over 5-HT(2A) ( approximately 4-fold). Several N- and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7e865895ecbc42acd8733dd4f39d674
https://doi.org/10.1016/s0960-894x(03)00403-7

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Differential pharmacology between the guinea-pig and the gorilla 5-HT1Dreceptor as probed with isochromans (5-HT1D-selective ligands)

Autor: Jeffrey F Pregenzer, Wha Bin Im, Glen L Alberts, Ennis Michael D, Robert Louis Hoffman, Tenbrink Ruth E, Jerry L. Slightom, Nabil B. Ghazal

Publikováno v: British Journal of Pharmacology. 127:468-472

Both the 5-HT1D and 5-HT1B receptors are implicated in migraine pathophysiology. Recently isochromans have been discovered to bind primate 5-HT1D receptors with much higher affinity than 5-HT1B receptors. In the guinea-pig, a primary animal model for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fe6ffa9681aa3bf271d60dc3bbb8e48e
https://doi.org/10.1038/sj.bjp.0702532

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Isochroman-6-carboxamides as Highly Selective 5-HT1D Agonists: Potential New Treatment for Migraine without Cardiovascular Side Effects

Autor: Robert B. McCall, Wha Bin Im, Kjell Svensson, Nabil B. Ghazal, Jeffrey F Pregenzer, Lorri T. Harris, Robert Louis Hoffman, Ennis Michael D, Lawson Cf, Martin W. Smith, Dorothy M. Sutter, Richard A. Lewis, Schlachter Sk, Edward D. Hall

Publikováno v: Journal of Medicinal Chemistry. 41:2180-2183

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3133ab586e8dce3e9c8b2da3ae17c0dc
https://doi.org/10.1021/jm980137o

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5-HT1D Receptor Agonist Properties of Novel 2-[5-[[(Trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and Their Use as Synthetic Intermediates

Autor: J. C. Mcguire, T. A. Barf, Nabil B. Ghazal, Håkan Wikström, S. J. Peroutka, Michael D. Ennis, Kjell A. Svensson, M. W. Smith, P. de Boer

Publikováno v: Journal of Medicinal Chemistry, 39(24), 4717-4726. AMER CHEMICAL SOC

2-[5-[[(Trifluoromethyl)sulfonyl]oxy]-1H-indol-3-yl]ethylamine (18), its N,N-di-n-propyl (12), N,N-diethyl (13), and N,N-dimethyl (14) derivatives, and 4-[3-[2-(N,N-dimethylamino)ethyl]1H-indol-3-yl]-N-(p-methoxybenzyl)acrylamide (GR46611, 19) were s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be345dc40bee68af626fe2973d98fbc5
https://doi.org/10.1021/jm9604890

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Structure-Activity Relationships in the 8-Amino-6,7,8,9-tetrahydro-3H-benz[e]indole Ring System. Part 2: Effect of 8-Amino Nitrogen Substitution on Serotonin Receptor Binding and Pharmacology

Autor: Chiu-Hong Lin, Håkan Wikström, Ennis, Stjernlöf P, Nabil B. Ghazal, Kjell A. Svensson, Robert Louis Hoffman, M. W. Smith, Haadsma-Svensson

Publikováno v: Journal of Medicinal Chemistry, 38(12), 2217-2230. AMER CHEMICAL SOC

A series of analogs of the potent and selective 5-HT1A agonist 8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1-carbaldehyde (2b) (OSU191) was prepared in which the dipropylamino group was modified to bear a variety of substituents. These c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1675e7c91edcdcbeb73466dbd9cde2df
https://doi.org/10.1021/jm00012a022

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Structure-Activity Relationships in the 8-Amino-6,7,8,9-tetrahydro-3H-benz[e]indole Ring System. Part 1: Effects of Substituents in the Aromatic System on Serotonin and Dopamine Receptor Subtypes

Autor: Robert Louis Hoffman, Stjernlöf P, Lars O. Hansson, Håkan Wikström, Arvid Carlsson, Ennis, Kjell A. Svensson, Nabil B. Ghazal, M. W. Smith, S. Sundell

Publikováno v: Journal of Medicinal Chemistry. 38:2202-2216

A series of 1-, 3-, and 4-substituted analogs to the potent 5-HT1A against 8-(dipropylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1-carbaldehyde (5) were prepared and tested in vitro at 5-HT1A, 5-HT1D alpha, 5-HT1D beta, D2, and D3 receptors and in vi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b768767d7aa42aaa34ab860911f16f73
https://doi.org/10.1021/jm00012a021

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The synthesis of (+)-and(−)-flesinoxan: Application of enzymatic resolution methodology

Autor: Nabil B. Ghazal, Michael D. Ennis

Publikováno v: Tetrahedron Letters. 33:6287-6290

The synthesis of (±)- flesinoxan was carried out in seven steps starting from catechol. An enzymatic resolution was utilized to prepare each enantiomer. Based upon the known preferences of the enzyme system used, we have assigned the (R)-configurati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9d438873d35ca8822f18a1ffecff606c
https://doi.org/10.1016/s0040-4039(00)60954-1

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