Search Results - "Mattson, Gail K."
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Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF1) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-05-2016)“…[Display omitted] A series of pyrazinone-based compounds incorporating either carbamate or aryl ether groups was synthesized and evaluated as…”
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Conformationally Restricted Homotryptamines. Part 7: 3-cis-(3-Aminocyclopentyl)indoles As Potent Selective Serotonin Reuptake Inhibitors
Published in Journal of medicinal chemistry (11-11-2010)“…A series of conformationally restricted homotryptamines has been synthesized and shown to be potent inhibitors of hSERT. Conformational restriction of the…”
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[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: Introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents
Published in Bioorganic & medicinal chemistry letters (01-11-2012)“…Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET…”
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Conformationally Restricted Homotryptamines. 2. Indole Cyclopropylmethylamines as Selective Serotonin Reuptake Inhibitors
Published in Journal of medicinal chemistry (22-09-2005)“…A series of indole cyclopropylmethylamines were found to be potent serotonin reuptake inhibitors. Nitrile substituents at the 5 and 7 positions of the indole…”
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Potential CRF1R PET imaging agents: 1-Fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones
Published in Bioorganic & medicinal chemistry letters (01-04-2013)“…A series of pyrazinones were prepared and evaluated as potential CRF1R PET imaging agents. Optimization of their CRF1R binding potencies and octanol–phosphate…”
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Conformationally restricted homotryptamines. Part 6: Indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors
Published in Bioorganic & medicinal chemistry letters (15-05-2013)“…Racemic 5-(trans-2-aminomethylcyclopropyl)indoles, 5-(trans-2-aminomethylcyclopentyl) indoles, and 5-(cis-2-aminomethylcyclopentyl)indoles were synthesized and…”
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Synthesis, Structure−Activity Relationships, and In Vivo Evaluation of N 3-Phenylpyrazinones as Novel Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists
Published in Journal of medicinal chemistry (23-07-2009)“…Evidence suggests that corticotropin-releasing factor-1 (CRF1) receptor antagonists may offer therapeutic potential for the treatment of diseases associated…”
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Potential CRF1R PET imaging agents: N-Fluoroalkyl-8-(6-methoxy-2-methyl-pyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines
Published in Bioorganic & medicinal chemistry letters (15-04-2011)“…A series of N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines were prepared and evaluated as…”
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Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors
Published in Bioorganic & medicinal chemistry letters (01-08-2009)“…A series of amines with structure 10 were synthesized and tested for inhibition of the human serotonin transporter (hSERT). A series of racemic…”
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Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors
Published in Bioorganic & medicinal chemistry letters (01-06-2007)“…A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were…”
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Synthesis and hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…A series of ring constrained homotryptamine analogs was prepared in 5 steps from 1-tosyl-3-vinylindoles via [3+2] dipolar cycloaddition with cyclic nitrones…”
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Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-03-2010)“…A series of N(3)-pyridylpyrazinones was investigated as corticotropin-releasing factor-1 receptor antagonists. It was observed that the binding affinity of…”
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Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor
Published in Bioorganic & medicinal chemistry letters (15-10-2007)“…Hybrid molecules containing the cyclopropylmethylamino side chain found in the parent homotryptamine system and an isosteric heteroaryl or naphthyl core were…”
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Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists
Published in Bioorganic & medicinal chemistry (15-08-2006)“…A series of novel 5,5-diphenylimidazolones was synthesized and evaluated for activity against the human neuropeptide Y5 receptor. The 3-pyridyl analog 46…”
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Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs)
Published in Bioorganic & medicinal chemistry letters (15-03-2005)“…A series of N, N-dimethylhomotryptamines was prepared and their binding affinities at the serotonin transporter (SERT) are reported. A series of N,…”
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Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (20-12-2004)“…4-Amino-N-arylpiperidines serve as effective bioisosteres for N-arylpiperazines in the series of dihydropyridine NPY1 receptor antagonists. These were prepared…”
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Differentially functionalized diamines as novel ligands for the NPY2 receptor
Published in Bioorganic & medicinal chemistry letters (01-09-2003)“…The synthesis of novel ligands for the NPY(2) receptor using solid phase split pool methodology is described. One of the analogues, diamine 16, was found to be…”
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Dihydropyridine neuropeptide Y Y1 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-02-2002)Get full text
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Synthesis and structure–activity relationships of N 3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF 1) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-03-2010)“…The structure–activity relationships of a series of N 3-pyridylpyrazinones as corticotropin-releasing factor-1 receptor antagonists was investigated. A series…”
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