- A new, simple procedure for the preparation of 8-methoxy-2-tetralone
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8-Methoxy-2-tetralone (6) can be easily prepared in approximately 50% overall yield starting from 2-bromophenylacetic acid (1), utilizing a Friedel-Crafts acylation/cyclization, ketone protection, copper(I)-catalyzed methoxylation of the aromatic bromide
- Lee,Frescas,Nichols
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- Novel [(diazomethyl)carbonyl]-1,2,3,4-tetrahydronaphthalene derivatives as potential photoaffinity ligands for the 5-HT(1A) receptor
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The photolabile (diazomethyl)carbonyl function was introduced into the 8-position of 2-(N,N-di-n-propyl-amino)-1,2,3,4-tetrahydronaphthalene in three ways, resulting in the ether 8-[[(diazomethyl)carbonyl]methoxy]-2-(N,N-di-n-propylamino)-1,2,3,4-te trahy
- Kline,Nelson,Namboodiri
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- The synthesis of (S)-di-n-propyl-(8-isoxazol-5-yl-1,2,3,4- tetrahydronaphthalen-2-yl)amine hydrochloride and its C-14-labeled isotopomer
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The partial ergoline LY228729 (1) which was a potent 5HT1A agonist has been studied clinically. Somewhat later, a related analog, (S)-di-n-propyl-(8-isoxazol-5-yl-1,2,3,4-tetrahydronaphthalen-2-yl)amine (2a) which in addition to potent 5HT
- Wheeler, William J.,O'Bannon, Douglas D.,Swanson, Steven,Gillespie, Todd A.,Varie, David L.
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- Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH2 at the human melanocortin-1 and -4 receptors: Histidine substitution
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Systematic substitution of His6 residue using non-selective hMC4R pentapeptide agonist (Bu-His6-DPhe7-Arg8-Trp9-Gly 10-NH2) as the template led to the identification of Bu-Atcsu
- Cheung, Adrian Wai-Hing,Danho, Waleed,Swistok, Joseph,Qi, Lida,Kurylko, Grazyna,Rowan, Karen,Yeon, Mitch,Franco, Lucia,Chu, Xin-Jie,Chen, Li,Yagaloff, Keith
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p. 133 - 137
(2007/10/03)
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- Antihyperglycemic Activity of Novel Naphthalenyl 3H-1,2,3,5-Oxathiadiazole 2-Oxides
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A series of naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus.Substitution at the 1-,5-, or 8-positions of the naphthalene ring with a halogen was found to be beneficial to antihyperglycemic activity. 4--3H-1,2,3,5-oxathiadiazole 2-oxide (45), one of the most potent compounds in this series, was selected for further pharmacological evaluation.
- Ellingboe, John W.,Lombardo, Louis J.,Alessi, Thomas R.,Nguyen, Thomas T.,Guzzo, Frieda,et al.
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p. 2485 - 2493
(2007/10/02)
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- Novel 2-substituted tetrahydro-3H-benz[e]indolamines: Highly potent and selective agonists acting at the 5-HT(1A) receptor as possible anxiolytics and antidepressants
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The synthesis of (+)-(R)-2-cyano-N,N-dipropyl-8-amino-6,7,8,9-tetrahydro- 3H-benz[e]indole [(R)-14, U92016A], a potent 5-HT(1A) agonist, and related analogs is described. In vitro binding studies show that the (R)-enantiomers of this series possess the hi
- Romero,Leiby,McCall,Piercey,Smith,Han
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p. 2066 - 2074
(2007/10/02)
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- 5-, 6-, 7- and 8-amino-2-(N,N-di-n-propylamino)-1,2,3,4-tetrahydrophthalenes: Centrally acting DA and 5-HT(1A) agonists
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5-, 6-, 7- and 8-Amino-2-(N,N-di-n-propylamino)-1,2,3,4-tetrahydronaphthalene were synthesized and compared with the corresponding phenolic compounds in vivo and in vitro for their effects on central serotonergic (5-HT(1A)) and dopaminergic (D2) systems. The 5- and 8-amino isomers surprisingly showed a 100-fold lower affinity for D2 and 5-HT(1A) receptors, respectively, than their corresponding phenols. This was also reflected in vivo. The 6-amino- and hydroxy-isomers were equipotent, while the 7-amino compound showed in vivo effects both on dopaminergic and serotonergic systems, the latter not being noticed in vitro. Intermediates 8-bromo-2-(N,N-di-n-propylamino)-1,2,3,4-tetrahydronaphthalene and 2-(N,N-di-n-propylamino)-1,2,3,4-tetrahydronaphthalene-8-carboxylic acid methyl ester were also tested and found to be quite potent 5-HT(1A) agonists.
- Stjernlof,Elebring,Andersson,Svensson,Svensson,Ekman,Carlsson,Wikstrom
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p. 693 - 701
(2007/10/02)
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- Novel naphthalenylalkyl-3H-1,2,3,5-oxathiadiazole 2-oxides useful as antihyperglycemic agents
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This invention relates to novel [(substituted naphthalenyl)alkyl]-3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical
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- Processes for the preparation of novel naphthalenylmethyl-3H-1,2,3,5-oxathiadiazole 2-oxides useful as antihyperglycemic agents
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This invention relates to the processes for the production of novel [(substituted naphthalenyl)methyl]-3H-1,2,3,5-oxathiadiazole 2-oxides. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and
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- 8-Substituted 2-aminotetralins
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New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
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