Search Results - "KONKEL, Michael J"
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Anxiolytic- and Antidepressant-like Profiles of the Galanin-3 Receptor ($Gal_3$) Antagonists SNAP 37889 and SNAP 398299
Published in Proceedings of the National Academy of Sciences - PNAS (29-11-2005)“…The neuropeptide galanin mediates its effects through the receptor subtypes$Gal_1$,$Gal_2$, and$Gal_3$and has been implicated in anxiety-and depression-related…”
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3-Arylimino-2-indolones Are Potent and Selective Galanin GAL3 Receptor Antagonists
Published in Journal of medicinal chemistry (29-06-2006)“…A series of 3-imino-2-indolones are the first published, high-affinity antagonists of the galanin GAL3 receptor. One example,…”
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Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal3 receptor binding affinity and improved solubility
Published in Bioorganic & medicinal chemistry letters (01-08-2006)“…A series of amino analogs of 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one (1) were synthesized to improve aqueous solubility, while…”
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Synthesis and Structure−Activity Relationship of Fluoro Analogues of 8-{2-[4-(4-Methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as Selective α1d-Adrenergic Receptor Antagonists
Published in Journal of medicinal chemistry (21-04-2005)“…We have discovered high-affinity antagonists (exemplified by 11 and 12) that are the most selective for α1d-adrenergic receptors (α1d-AR) reported to date. In…”
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Palladium-Catalyzed Allylic Coupling of 1,2,3-Triazolo[4,5-d]pyrimidines (8-Azapurines)
Published in Journal of organic chemistry (06-09-1996)“…The palladium-catalyzed coupling of the sodium salt of 7-amino-1,2,3-triazolo[4,5-d]pyrimidine (8-azaadenine, 1) with allylic phosphates or carbonates resulted…”
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Structure Determination of the Products from the Acid-Catalyzed Condensation of Indole with Acetone
Published in Journal of organic chemistry (26-01-1996)“…Four of the previously reported compounds obtained from the acid-catalyzed condensation of indole with acetone are now assigned the following structures: …”
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Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists
Published in Journal of medicinal chemistry (21-04-2005)“…We have discovered high-affinity antagonists (exemplified by 11 and 12) that are the most selective for alpha(1d)-adrenergic receptors (alpha(1d)-AR) reported…”
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Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal 3 receptor binding affinity and improved solubility
Published in Bioorganic & medicinal chemistry letters (2006)“…A series of amino analogs of 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2 H-indol-2-one ( 1) were synthesized to improve aqueous solubility,…”
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Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal sub(3) receptor binding affinity and improved solubility
Published in Bioorganic & medicinal chemistry letters (01-01-2006)“…A series of amino analogs of 1,3-dihydro-1-phenyl-3-[[3- (trifluoromethyl)phenyl]imino]-2H-indol-2-one (1) were synthesized to improve aqueous solubility,…”
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3-Arylimino-2-indolones Are Potent and Selective Galanin GAL 3 Receptor Antagonists
Published in Journal of medicinal chemistry (01-06-2006)Get full text
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3-arylimino-2-indolones are potent and selective galanin GAL3receptor antagonists
Published in Journal of medicinal chemistry (2006)Get full text
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Cyclohexenyl nucleosides: Synthesis of cis-4-(9 H-purin-9-yl)-2-cyclohexenylcarbinols
Published in Tetrahedron (15-01-1996)“…Syntheses of the title compounds were accomplished in 6–7 steps, starting from cyclohexadiene and chlorosulphonyl isocyanate. The key step of the strategy…”
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Cyclohexenyl nucleosides: Synthesis and biological activity of trans-3-(purin-9-yl)-4-cyclohexenylcarbinols
Published in Tetrahedron (01-07-1996)“…The primary alcohol of cis-3-hydroxy-4-cyclohexenylcarbinol was protected with a silyl group and then the configuration of the secondary alcohol was inverted…”
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In situ vinylindole synthesis. Diels-Alder reactions with maleic anhydride and maleic acid to give tetrahydrocarbazoles and carbazoles
Published in Tetrahedron (25-03-1996)“…Tetrahydrocarbazoles have been prepared in one-flask syntheses from indoles, ketones, and maleic anhydride, with acid catalysis. The reactions involve a…”
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In situ vinylindole synthesis. Diels-alder reactions with maleimides to give tetrahydrocarbazoles
Published in Journal of heterocyclic chemistry (01-01-1993)“…Tetrahydrocarbazoles have been prepared in one‐flask syntheses from indoles, ketones or aldehydes, and maleimides, with acid catalysis. The reactions involve a…”
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Diels-alder reactions of 3-(2-nitrovinyl)indoles: Formation of carbazoles and bridged carbazoles
Published in Journal of heterocyclic chemistry (01-01-1993)“…The Diels‐Alder reactions of 1‐substituted‐3‐(2‐nitrovinyl)indoles 3 with quinones and acetylenes give aromatized 1:1 adducts (‐ nitrous acid) (1) or (‐…”
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