Search Results - "McCarthy, James R"
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Totally Endoscopic Robotic Mitral Valve Surgery
Published in AORN journal (01-10-2016)“…Abstract Mitral valve dysfunction can seriously impair patients’ lives and may require valve repair or replacement. Surgery can be performed using techniques…”
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Potent, Orally Active Corticotropin-Releasing Factor Receptor-1 Antagonists Containing a Tricyclic Pyrrolopyridine or Pyrazolopyridine Core
Published in Journal of medicinal chemistry (16-06-2005)“…Two new classes of tricyclic-based corticotropin-releasing factor (CRF1) receptor-1 antagonists were designed by constraining known 1H-pyrrolo[2,3-b]pyridine…”
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3
Design and synthesis of statine-containing BACE inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2003)“…Utilizing structure-based techniques and solid-phase synthesis, statine-based tetrapeptide BACE inhibitors were designed and synthesized using a heptapeptide…”
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4
Urocortin shares the memory modulating effects of corticotropin-releasing factor (CRF): mediation by CRF1 receptors
Published in Brain research (18-10-2002)“…Intracerebroventricular (i.c.v.) administration of corticotropin-releasing factor (CRF) biphasically affects performance in tests of learning and memory. In…”
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5
Mitsunobu Approach to the Synthesis of Optically Active α,α-Disubstituted Amino Acids
Published in Organic letters (19-02-2009)“…Chiral tertiary α-hydroxy esters of known stereochemical configuration were transformed to α-azido esters by Mitsunobu reaction with HN3. Optimization of this…”
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6
Optimization of Hydroxyethylamine Transition State Isosteres as Aspartic Protease Inhibitors by Exploiting Conformational Preferences
Published in Journal of medicinal chemistry (14-12-2017)“…NMR conformational analysis of a hydroxyethylamine peptide isostere developed as an aspartic protease inhibitor shows that it is a flexible architecture…”
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Design and Synthesis of a Series of Non-Peptide High-Affinity Human Corticotropin-Releasing Factor1 Receptor Antagonists
Published in Journal of medicinal chemistry (25-10-1996)Get full text
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8
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (06-10-2003)“…A series of 4-substituted 8-aryl-2-methylquinolines 4 was designed and synthesized as highly potent antagonists for the human CRF(1) receptor. This series of…”
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9
Synthesis, Crystallization, and Biological Evaluation of an Orally Active Prodrug of Gemcitabine
Published in Journal of medicinal chemistry (26-11-2009)“…The design, synthesis, and biological characterization of an orally active prodrug (3) of gemcitabine are described. Additionally, the identification of a…”
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Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylamino-pyrazolo[1,5-a] pyrimidine (NBI 30775/r121919) and structure-activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists
Published in Journal of medicinal chemistry (09-09-2004)Get full text
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11
Inactivation of Ribonucleotide Reductase by (E)-2‘-Fluoromethylene-2‘-deoxycytidine 5‘-Diphosphate: A Paradigm for Nucleotide Mechanism-Based Inhibitors
Published in Biochemistry (Easton) (25-06-1996)“…Ribonucleotide reductase (RDPR) from Escherichia coli catalyzes the conversion of nucleotides to deoxynucleotides and is composed of two homodimeric subunits: …”
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12
Cyclopropanecarboxylic Acid Esters as Potential Prodrugs with Enhanced Hydrolytic Stability
Published in Organic letters (07-02-2008)“…Esters of cyclopropanecarboxylic acid demonstrate a substantial increase in stability under both acid- and base-catalyzed hydrolytic conditions. Comparison of…”
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13
Application of the Dakin−West Reaction for the Synthesis of Oxazole-Containing Dual PPARα/γ Agonists
Published in Journal of organic chemistry (04-04-2003)“…An improved method for the preparation of a series of oxazole-containing dual PPARα/γ agonists is described. A synthetic sequence utilizing a Dakin−West…”
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14
Terminal difluoro olefin analogs of squalene are time-dependent inhibitors of squalene epoxidase
Published in Journal of the American Chemical Society (01-01-1992)Get full text
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15
A tailored therapy for the metabolic syndrome: The dual peroxisome proliferator-activated receptor-α/γ agonist LY465608 ameliorates insulin resistance and diabetic hyperglycemia while improving cardiovascular risk factors in preclinical models
Published in Diabetes (New York, N.Y.) (01-04-2002)“…A novel nonthiazolidinedione dual peroxisome proliferator- activated receptor (PPAR)-alpha/gamma agonist, LY465608, was designed to address the major metabolic…”
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Macrocyclic peptidomimetic inhibitors of β-secretase (BACE): First X-ray structure of a macrocyclic peptidomimetic-BACE complex
Published in Bioorganic & medicinal chemistry letters (2006)“…The synthesis of novel macrocyclic peptidomimetic inhibitors of BACE1 is described. These macrocycles are derived from a hydroxyethylene core structure…”
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17
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility
Published in Bioorganic & medicinal chemistry letters (16-07-2004)“…In our efforts to identify potent CRF(1) antagonists with proper physicochemical properties, a series of 3-phenylpyrazolo[1,5-a]pyrimidines bearing polar…”
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18
A convenient synthesis of the antibacterial agent linezolid
Published in Tetrahedron letters (09-12-2015)“…[Display omitted] Starting with 3,4-difluorobenzoic acid (8) and (S)-epichlorohydrin (13) a convergent synthesis of linezolid (1) was developed that is…”
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Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (02-08-2004)“…A series of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines was designed and synthesized as antagonists for the corticotrophin-releasing factor-1 (CRF(1)) receptor…”
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Rational Design, Synthesis, and Structure−Activity Relationships of Aryltriazoles as Novel Corticotropin-Releasing Factor-1 Receptor Antagonists
Published in Journal of medicinal chemistry (10-03-2005)“…Following the discovery of the very high binding affinity of 4-anilinopyrimidines against corticotropin-releasing factor receptor-1 (CRF1) (e.g., 1, K i = 2…”
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