Search Results - "Eckman, Joseph"
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Preclinical Experimental and Mathematical Approaches for Assessing Effective Doses of Inhaled Drugs, Using Mometasone to Support Human Dose Predictions
Published in Journal of aerosol medicine and pulmonary drug delivery (01-08-2016)“…Understanding the relationship between dose, lung exposure, and drug efficacy continues to be a challenging aspect of inhaled drug development. An experimental…”
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LBY135, a novel anti-DR5 agonistic antibody induces tumor cell-specific cytotoxic activity in human colon tumor cell lines and xenografts
Published in Drug development research (01-03-2008)“…TRAIL (TNF‐related apoptosis‐inducing ligand) induces apoptosis on binding to DR4 and DR5 receptors on the surface of tumor cells. These receptors are of…”
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5-Lipoxygenase inhibitors with histamine H1 receptor antagonist activity
Published in Bioorganic & medicinal chemistry letters (03-05-2004)Get full text
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5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds
Published in Bioorganic & medicinal chemistry letters (15-02-2005)“…A series of N-hydroxycarbamates containing a histaminergic H 1 receptor antagonist pharmacophore was synthesized. The compounds possessed both…”
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Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity
Published in Bioorganic & medicinal chemistry letters (15-11-2004)“…Three different histaminergic H 1 scaffolds were attached by various linkers to a single 5-LO scaffold. Both activities were observed in vitro. Pharmacokinetic…”
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Anti-inflammatory actions of Chemoattractant Receptor-homologous molecule expressed on Th2 by the antagonist MK-7246 in a novel rat model of Alternaria alternata elicited pulmonary inflammation
Published in European journal of pharmacology (15-11-2014)“…Alternaria alternata is a fungal allergen linked to the development of severe asthma in humans. In view of the clinical relationship between A. alternata and…”
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Alternaria alternata induced inflammatory lung responses: a novel in vivo PK/PD model
Published in Journal of inflammation (London, England) (14-08-2013)“…Doc number: P10…”
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Efficacy of Panobinostat (LBH589) in Multiple Myeloma Cell Lines and In Vivo Mouse Model: Tumor-Specific Cytotoxicity and Protection of Bone Integrity in Multiple Myeloma
Published in Blood (16-11-2007)“…Panobinostat (LBH589) is a highly potent oral pan-deacetylase (DAC) inhibitor currently undergoing clinical development in hematologic and solid malignancies…”
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5-Lipoxygenase inhibitors with histamine H 1 receptor antagonist activity
Published in Bioorganic & medicinal chemistry letters (03-05-2004)Get full text
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Epibatidine is a nicotinic analgesic
Published in European journal of pharmacology (21-12-1993)“…Epibatidine, an alkaloid isolated from skin of the poison frog, Epipedobates tricolor, has been shown to be a very potent analgesic with a non-opioid mechanism…”
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Synthesis and screening of a combinatorial library of naphthalene substituted chalcones: inhibitors of leukotriene B 4
Published in Bioorganic & medicinal chemistry (01-06-1999)“…A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leukotriene B…”
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Synthesis and screening of a combinatorial library of naphthalene substituted chalcones : Inhibitors of leukotriene B4
Published in Bioorganic & medicinal chemistry (01-06-1999)“…A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leukotriene B4…”
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5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity
Published in Bioorganic & medicinal chemistry letters (03-05-2004)“…A series of novel compounds with both 5-lipoxygenase (5-LO) inhibitory and histamine H(1) receptor antagonist activity were designed for the treatment of…”
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(±)-trans-2-[3-Methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a Potent Dual 5-Lipoxygenase Inhibitor and Platelet-Activating Factor Receptor Antagonist
Published in Journal of medicinal chemistry (21-05-1998)“…By incorporating an N-hydroxyurea functionality onto diaryltetrahydrofurans, a novel series of compounds was investigated as dual 5-lipoxygenese (5-LO)…”
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Cmi-206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor
Published in Bioorganic & medicinal chemistry letters (16-03-1995)“…CMI-206, trans-2[3-methoxy-4-propoxy-5(N′-butyl-N′-hydroxyureidyl)phenyl]-5-(3,4,5-trimethoxyphenyl) tetrahydrofuran, was synthesized and was found to…”
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