Search Results - "Krueger, JA"
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Olanzapine versus haloperidol in the treatment of schizophrenia and schizoaffective and schizophreniform disorders: results of an international collaborative trial
Published in The American journal of psychiatry (01-04-1997)“…OBJECTIVE: This international, multicenter double-blind trial was designed to compare the therapeutic profile of an atypical antipsychotic, olanzapine, with…”
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Spontaneous sleep in mice with targeted disruptions of neuronal or inducible nitric oxide synthase genes
Published in Brain research (30-05-2003)“…Nitric oxide (NO) affects almost every physiological process, including the regulation of sleep. There is strong evidence that NO plays an important role in…”
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Discovery and Evaluation of Potent P 1 Aryl Heterocycle-Based Thrombin Inhibitors
Published in Journal of medicinal chemistry (03-06-2004)Get full text
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Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization
Published in Bioorganic & medicinal chemistry letters (15-10-2005)“…Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin…”
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9-Hydroxyazafluorenes and Their Use in Thrombin Inhibitors
Published in Journal of medicinal chemistry (07-04-2005)“…Optimization of a previously reported thrombin inhibitor, 9-hydroxy-9-fluorenylcarbonyl-l-prolyl-trans-4-aminocyclohexylmethylamide (1), by replacing the…”
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The extent and distribution of cell death and matrix damage in impacted chondral explants varies with the presence of underlying bone
Published in Journal of biomechanical engineering (01-02-2003)“…Excessive mechanical loading can lead to matrix damage and chondrocyte death in articular cartilage. Previous studies on chondral and osteochondral explants…”
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Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles
Published in Bioorganic & medicinal chemistry letters (15-01-2006)“…Imidazoles and aminothiazoles, in spite of their weak basicity, have been optimized to function as potent P1 ligands in both a peptide series and a nonpeptide…”
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Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the ‘Distal binding pocket’
Published in Bioorganic & medicinal chemistry letters (20-01-2003)“…Use of a chlorophenoxyacetamide P1 group with a pyridinone acetamide P2/P3 gave an exceptionally potent thrombin inhibitor ( K i=40 pM). Truncation of the…”
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P 2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold
Published in Bioorganic & medicinal chemistry letters (02-06-2005)“…In this study, we demonstrate that the critical hydrogen bonding motif of the established 3-aminopyrazinone thrombin inhibitors can be effectively mimicked by…”
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Cyclopropylamino Acid Amide as a Pharmacophoric Replacement for 2,3-Diaminopyridine. Application to the Design of Novel Bradykinin B sub(1) Receptor Antagonists
Published in Journal of medicinal chemistry (23-02-2006)“…Antagonism of the bradykinin B sub(1) receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists were designed that display…”
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Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position
Published in Bioorganic & medicinal chemistry letters (20-10-2003)“…Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in…”
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Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (10-03-2003)“…Starting from a 2-amino-6-methylpyridine P1 group and following a strategy of enlarging it whilst reducing its polarity, we have developed a series of potent,…”
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Design and synthesis of potent and selective macrocyclic thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (18-08-2003)“…A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. Detailed SAR studies led to the incorporation of…”
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Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability
Published in Bioorganic & medicinal chemistry letters (16-08-2004)“…In order to overcome several limitations of our lead compound, which possessed a fluorenyl side chain in P3, we synthesized a series of analogs where we…”
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Growth and injury patterns of eastern white pine (Pinus strobus L.) seedlings as affected by hardwood overstory density and weeding treatments
Published in Northern Journal of Applied Forestry (01-06-2004)“…White pine seedlings were underplanted under a range of overstory densities in a hardwood stand in northern Minnesota. Vegetation surrounding seedlings was…”
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L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor
Published in Bioorganic & medicinal chemistry letters (07-04-1998)“…Replacement of the amidinopiperidine P1 group of 3-benzylsulfonylamino-6-methyl-2-pyridinone acetamide thrombin inhibitor L-373,890 ( 2) with a mildly basic…”
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3-Amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (17-04-2003)“…We describe a series of highly potent and efficacious thrombin inhibitors based on a 3-amino-4-sulfonylpyridinone acetamide template. The functionally dense…”
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Early growth responses of naturally regenerated eastern white pine (Pinus strobus L.) to partial release from juvenile aspen and pathological pruning
Published in Northern Journal of Applied Forestry (01-03-2005)“…Height, breast height diameter, and basal diameter growth responses of 7- to 12-year-old naturally regenerated eastern white pine (Pinus strobus L.) to partial…”
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Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors
Published in Bioorganic & medicinal chemistry letters (15-05-2000)“…A new class of conformationally constrained thrombin inhibitors is described. These compounds contain a unique bicyclic pyridone scaffold which serves as a…”
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