Search Results - "Walker, Keith A."
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Novel Series of Dihydropyridinone P2X7 Receptor Antagonists
Published in Journal of medicinal chemistry (12-11-2015)“…Identification of singleton P2X7 inhibitor 1 from HTS gave a pharmacophore that eventually turned into potential clinical candidates 17 and 19. During…”
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2
Oligonucleotide-Mediated Genome Editing Provides Precision and Function to Engineered Nucleases and Antibiotics in Plants
Published in Plant physiology (Bethesda) (01-04-2016)“…Here, we report a form of oligonucleotide-directed mutagenesis for precision genome editing in plants that uses single-stranded oligonucleotides (ssODNs) to…”
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3
Oligonucleotide‐directed mutagenesis for precision gene editing
Published in Plant biotechnology journal (01-02-2016)“…Differences in gene sequences, many of which are single nucleotide polymorphisms, underlie some of the most important traits in plants. With humanity facing…”
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4
Lactams as EP4 Prostanoid Receptor Agonists. 3. Discovery of N-Ethylbenzoic Acid 2-Pyrrolidinones as Subtype Selective Agents
Published in Journal of medicinal chemistry (02-12-2004)“…Two distinct synthetic schemes were applied to access heteroatom-containing α-chain lactams or lactams terminated as aryl acids. The latter lactams were…”
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Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism
Published in Bioorganic & medicinal chemistry letters (01-06-2010)“…A series of 5-HT6 ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several neutral, non-basic analogs having…”
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6
Stereoisomers of ketoconazole: preparation and biological activity
Published in Journal of medicinal chemistry (01-07-1992)“…The four stereoisomers of the antifungal agent ketoconazole (1) were prepared and evaluated for their selectivity in inhibiting a number of cytochrome P-450…”
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7
Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors
Published in Bioorganic & medicinal chemistry letters (20-09-2004)“…The introduction of 3-arylmethyl, 3-aryloxy and 3-arylthio moieties into a 6-methylsulfonylindole framework using rational drug design led to potent, selective…”
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A revised mechanism for the Mitsunobu reaction
Published in Journal of organic chemistry (01-09-1987)Get full text
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9
Design and synthesis of orally active inhibitors of TNF synthesis as anti-rheumatoid arthritis drugs
Published in Bioorganic & medicinal chemistry letters (17-11-2003)“…A novel series of TNF inhibitors was identified based on the screening of existing MMP inhibitor libraries. Further SAR optimization led to the discovery of a…”
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10
Amino acid derived sulfonamide hydroxamates as inhibitors of procollagen C-proteinase. Part 2: Solid-phase optimization of side chains
Published in Bioorganic & medicinal chemistry letters (22-04-2002)“…Optimization of the amino acid side chain and the N-alkyl group of the sulfonamide of amino acid derived sulfonamide hydroxamates is discussed. The solid-phase…”
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11
Somatic seeds: encapsulation of asexual plant embryos
Published in Bio/technology (New York, N.Y. 1983) (01-09-1986)Get full text
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12
Synthesis of analogs of prostacyclin containing a thiazole ring
Published in Journal of organic chemistry (01-05-1983)Get full text
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13
3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase
Published in Journal of medicinal chemistry (01-02-1992)“…A series of 1H-imidazol-1-yl- and 3-pyridyl-substituted 3,4-dihydroquinolin-2(1H)-ones was designed and synthesized as combined inhibitors of thromboxane…”
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14
Antitrichomonal activity of mesoionic thiazolo[3,2-a]pyridines
Published in Journal of medicinal chemistry (01-11-1985)“…Screening of mesoionic compounds as potential electron acceptors by analogy with metronidazole led to the finding of in vitro antitrichomonal activity for…”
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15
Stereochemical Consequences of 6- and 8-Substitution in Reactions of Bicyclo[4.2.0]octan-7-ones
Published in Journal of organic chemistry (01-03-1994)Get full text
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16
Effects of 16-heterosubstitution on the regiochemistry of the D-homo rearrangement
Published in Journal of organic chemistry (01-09-1985)Get full text
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17
Selective Inhibition of Mammalian Lanosterol 14.alpha.-Demethylase by RS-21607 in vitro and in vivo
Published in Biochemistry (Easton) (01-04-1994)Get full text
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18
Unexpected cis-openings of cyclopentadiene monoepoxide with lithium acetylides and dialkylalkynylalanes
Published in Journal of organic chemistry (01-04-1990)Get full text
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19
Selective inhibition of mammalian lanosterol 14.alpha.-demethylase: a possible strategy for cholesterol lowering
Published in Journal of medicinal chemistry (01-07-1993)Get full text
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Highly potent, non-basic 5-HT sub(6) ligands. Site mutagenesis evidence for a second binding mode at 5-HT sub(6) for antagonism
Published in Bioorganic & medicinal chemistry letters (01-06-2010)“…A series of 5-HT sub(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having…”
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