Expert Opinion on Therapeutic Patents, ISSN 1354-3776, 01/2009, Volume 19, Issue 1, pp. 39 - 58
Background: Chemokines were originally defined as host defense proteins, however, their biological role goes well beyond this simple description of their...
chemokine receptors | antagonism | chemokines | GPCRs | Antagonism | Chemokine receptors | Chemokines | RHEUMATOID-ARTHRITIS | ALLOGRAFT-REJECTION | SELECTIVE ANTAGONIST | CHEMISTRY, MEDICINAL | PROTEIN-COUPLED RECEPTORS | POTENT CCR2 ANTAGONISTS | BIPIPERIDINE AMIDE COMPOUNDS | PIPERIDINE-DERIVATIVES | FUNCTIONAL EXPRESSION | IN-VIVO | PHARMACOLOGY & PHARMACY | SMALL-MOLECULE ANTAGONISTS | Animals | Humans | Drug Design | Patents as Topic | Chemokines, CC - metabolism | Drug Delivery Systems | Receptors, CCR1 - antagonists & inhibitors | Receptors, CCR2 - antagonists & inhibitors | Receptors, CCR3 - antagonists & inhibitors | Receptors, CCR4 - antagonists & inhibitors
chemokine receptors | antagonism | chemokines | GPCRs | Antagonism | Chemokine receptors | Chemokines | RHEUMATOID-ARTHRITIS | ALLOGRAFT-REJECTION | SELECTIVE ANTAGONIST | CHEMISTRY, MEDICINAL | PROTEIN-COUPLED RECEPTORS | POTENT CCR2 ANTAGONISTS | BIPIPERIDINE AMIDE COMPOUNDS | PIPERIDINE-DERIVATIVES | FUNCTIONAL EXPRESSION | IN-VIVO | PHARMACOLOGY & PHARMACY | SMALL-MOLECULE ANTAGONISTS | Animals | Humans | Drug Design | Patents as Topic | Chemokines, CC - metabolism | Drug Delivery Systems | Receptors, CCR1 - antagonists & inhibitors | Receptors, CCR2 - antagonists & inhibitors | Receptors, CCR3 - antagonists & inhibitors | Receptors, CCR4 - antagonists & inhibitors
Journal Article
The Journal of Allergy and Clinical Immunology, ISSN 0091-6749, 02/2019, Volume 143, Issue 2, pp. 669 - 680.e12
Chemokine signaling through CCR3 is a key regulatory pathway for eosinophil recruitment into tissues associated with allergic inflammation and asthma. To date,...
airway hyperresponsiveness | allergic inflammation | biased antagonist | asthma | eosinophil | CCR3 | peptide nanoparticles | ACTIVATION | PROTEIN | CXCR4 ANTAGONIST | CELL-SURFACE | BETA-ARRESTIN | IMMUNOLOGY | CHEMOKINE RECEPTOR CCR3 | ALLERGY | DEGRANULATION | UP-REGULATION | EOTAXIN | EXPRESSION
airway hyperresponsiveness | allergic inflammation | biased antagonist | asthma | eosinophil | CCR3 | peptide nanoparticles | ACTIVATION | PROTEIN | CXCR4 ANTAGONIST | CELL-SURFACE | BETA-ARRESTIN | IMMUNOLOGY | CHEMOKINE RECEPTOR CCR3 | ALLERGY | DEGRANULATION | UP-REGULATION | EOTAXIN | EXPRESSION
Journal Article
Medicinal Research Reviews, ISSN 0198-6325, 09/2010, Volume 30, Issue 5, pp. 778 - 817
The chemokine receptor CCR3 is believed to play a role in the development of allergic diseases such as asthma, atopic dermatitis, and allergic rhinitis....
antagonists | allergic disease | CCR3 | chemokine receptor | low‐molecular‐weight | Antagonists | Chemokine receptor | Low-molecular-weight | Allergic disease | SELECTIVE ANTAGONIST | CHEMISTRY, MEDICINAL | low-molecular-weight | DISCOVERY | BIPIPERIDINE AMIDE COMPOUNDS | RIGID CYCLIC TEMPLATES | INTERNATIONAL UNION | IN-VIVO | ASTHMA | PHARMACOLOGY & PHARMACY | PART 1 | AIRWAY HYPERRESPONSIVENESS | STABILIZED ACYCLIC SCAFFOLDS | Amino Acid Sequence | Small Molecule Libraries - chemistry | Small Molecule Libraries - pharmacology | Animals | Humans | Molecular Sequence Data | Structure-Activity Relationship | Receptors, CCR3 - chemistry | Receptors, CCR3 - antagonists & inhibitors | Patents | amides | Calcium (intracellular) | Phenylalanine | Hypersensitivity | Leukocytes (eosinophilic) | piperazine | Allergic diseases | Inflammation | Structure-activity relationships | Chemotaxis | Chemokine receptors | Asthma | Urea | Atopic dermatitis | Allergic rhinitis
antagonists | allergic disease | CCR3 | chemokine receptor | low‐molecular‐weight | Antagonists | Chemokine receptor | Low-molecular-weight | Allergic disease | SELECTIVE ANTAGONIST | CHEMISTRY, MEDICINAL | low-molecular-weight | DISCOVERY | BIPIPERIDINE AMIDE COMPOUNDS | RIGID CYCLIC TEMPLATES | INTERNATIONAL UNION | IN-VIVO | ASTHMA | PHARMACOLOGY & PHARMACY | PART 1 | AIRWAY HYPERRESPONSIVENESS | STABILIZED ACYCLIC SCAFFOLDS | Amino Acid Sequence | Small Molecule Libraries - chemistry | Small Molecule Libraries - pharmacology | Animals | Humans | Molecular Sequence Data | Structure-Activity Relationship | Receptors, CCR3 - chemistry | Receptors, CCR3 - antagonists & inhibitors | Patents | amides | Calcium (intracellular) | Phenylalanine | Hypersensitivity | Leukocytes (eosinophilic) | piperazine | Allergic diseases | Inflammation | Structure-activity relationships | Chemotaxis | Chemokine receptors | Asthma | Urea | Atopic dermatitis | Allergic rhinitis
Journal Article
Nature, ISSN 0028-0836, 07/2009, Volume 460, Issue 7252, pp. 225 - 230
Age-related macular degeneration (AMD), a leading cause of blindness worldwide, is as prevalent as cancer in industrialized nations. Most blindness in AMD...
EOSINOPHIL RECRUITMENT | VISUAL FUNCTION | VEGF | MULTIDISCIPLINARY SCIENCES | MAST-CELLS | GENE-EXPRESSION PROFILES | EXPERIMENTAL CHOROIDAL NEOVASCULARIZATION | MODEL | EOTAXIN | ENDOTHELIAL GROWTH-FACTOR | RETINAL-PIGMENT EPITHELIUM | Retina - drug effects | Choroidal Neovascularization - diagnosis | Cell Proliferation | Receptors, CCR3 - immunology | Humans | Chemokine CCL24 - metabolism | Leukocytes | Vascular Endothelial Growth Factor A - antagonists & inhibitors | Chemokine CCL26 | Macular Degeneration - diagnosis | Choroid - cytology | Chemokine CCL11 - antagonists & inhibitors | Receptors, CCR3 - genetics | Disease Models, Animal | Receptors, CCR3 - antagonists & inhibitors | Choroid - metabolism | Chemokine CCL11 - metabolism | Endothelial Cells - metabolism | Mice, Inbred C57BL | Cells, Cultured | Choroid - blood supply | Vascular Endothelial Growth Factor A - immunology | Inflammation | Chemokines, CC - antagonists & inhibitors | Macular Degeneration - metabolism | Receptors, CCR3 - metabolism | Animals | Chemokine CCL24 - antagonists & inhibitors | Choroidal Neovascularization - metabolism | Macular Degeneration - therapy | Quantum Dots | Endothelial Cells - cytology | Receptors, CCR3 - analysis | Ligands | Mice | Retina - pathology | Cell Movement | Chemokines, CC - metabolism | Macular degeneration | Physiological aspects | Care and treatment | Genetic aspects | Chemokine receptors | Ophthalmology | Quantum dots | Cells | Index Medicus
EOSINOPHIL RECRUITMENT | VISUAL FUNCTION | VEGF | MULTIDISCIPLINARY SCIENCES | MAST-CELLS | GENE-EXPRESSION PROFILES | EXPERIMENTAL CHOROIDAL NEOVASCULARIZATION | MODEL | EOTAXIN | ENDOTHELIAL GROWTH-FACTOR | RETINAL-PIGMENT EPITHELIUM | Retina - drug effects | Choroidal Neovascularization - diagnosis | Cell Proliferation | Receptors, CCR3 - immunology | Humans | Chemokine CCL24 - metabolism | Leukocytes | Vascular Endothelial Growth Factor A - antagonists & inhibitors | Chemokine CCL26 | Macular Degeneration - diagnosis | Choroid - cytology | Chemokine CCL11 - antagonists & inhibitors | Receptors, CCR3 - genetics | Disease Models, Animal | Receptors, CCR3 - antagonists & inhibitors | Choroid - metabolism | Chemokine CCL11 - metabolism | Endothelial Cells - metabolism | Mice, Inbred C57BL | Cells, Cultured | Choroid - blood supply | Vascular Endothelial Growth Factor A - immunology | Inflammation | Chemokines, CC - antagonists & inhibitors | Macular Degeneration - metabolism | Receptors, CCR3 - metabolism | Animals | Chemokine CCL24 - antagonists & inhibitors | Choroidal Neovascularization - metabolism | Macular Degeneration - therapy | Quantum Dots | Endothelial Cells - cytology | Receptors, CCR3 - analysis | Ligands | Mice | Retina - pathology | Cell Movement | Chemokines, CC - metabolism | Macular degeneration | Physiological aspects | Care and treatment | Genetic aspects | Chemokine receptors | Ophthalmology | Quantum dots | Cells | Index Medicus
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2012, Volume 22, Issue 22, pp. 6876 - 6881
Optimization starting with our lead compound (IC = 4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward...
Pyrrolidinyl phenylurea derivatives | Allergic diseases | CCR3 antagonists | POTENT | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | PART 1 | UREA DERIVATIVES | DISCOVERY | Administration, Oral | Pyrrolidines - pharmacokinetics | Half-Life | Macaca fascicularis | Biological Availability | Pyrrolidines - chemistry | Receptors, CCR3 - metabolism | Animals | Phenylurea Compounds - chemical synthesis | Pyrrolidines - chemical synthesis | Phenylurea Compounds - chemistry | Phenylurea Compounds - pharmacokinetics | Receptors, CCR3 - antagonists & inhibitors
Pyrrolidinyl phenylurea derivatives | Allergic diseases | CCR3 antagonists | POTENT | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | PART 1 | UREA DERIVATIVES | DISCOVERY | Administration, Oral | Pyrrolidines - pharmacokinetics | Half-Life | Macaca fascicularis | Biological Availability | Pyrrolidines - chemistry | Receptors, CCR3 - metabolism | Animals | Phenylurea Compounds - chemical synthesis | Pyrrolidines - chemical synthesis | Phenylurea Compounds - chemistry | Phenylurea Compounds - pharmacokinetics | Receptors, CCR3 - antagonists & inhibitors
Journal Article
Clinical & Experimental Allergy, ISSN 0954-7894, 04/2014, Volume 44, Issue 4, pp. 508 - 516
Summary Background Several chemokines, notably eotaxin, mediate the recruitment of eosinophils into tissues via the CCR3 receptor. Objective In this study, we...
clinical trial | sputum eosinophils | eotaxin | asthma | CCR3 | Clinical trial | Sputum eosinophils | Eotaxin | Asthma | PROGENITORS | EOTAXIN RECEPTOR CCR3 | SPUTUM | MAST-CELLS | ALLERGEN | IMMUNOLOGY | INTERLEUKIN-5 | HYPERRESPONSIVENESS | PATHOGENESIS | ALLERGY | ACCUMULATION | EXPRESSION | Sputum - cytology | Humans | Middle Aged | Male | Eosinophils - immunology | Young Adult | Sputum - immunology | Benzamides - therapeutic use | Adult | Bronchitis - complications | Female | Benzamides - pharmacology | Eosinophils - pathology | Leukocyte Count | Receptors, CCR3 - antagonists & inhibitors | Asthma - physiopathology | Treatment Outcome | Bronchitis - physiopathology | Asthma - drug therapy | Methylurea Compounds - pharmacology | Methylurea Compounds - therapeutic use | Bronchitis - drug therapy | Pulmonary Eosinophilia - complications | Aged | Respiratory Function Tests | Chemotaxis, Leukocyte - immunology | Clinical trials | Bronchitis
clinical trial | sputum eosinophils | eotaxin | asthma | CCR3 | Clinical trial | Sputum eosinophils | Eotaxin | Asthma | PROGENITORS | EOTAXIN RECEPTOR CCR3 | SPUTUM | MAST-CELLS | ALLERGEN | IMMUNOLOGY | INTERLEUKIN-5 | HYPERRESPONSIVENESS | PATHOGENESIS | ALLERGY | ACCUMULATION | EXPRESSION | Sputum - cytology | Humans | Middle Aged | Male | Eosinophils - immunology | Young Adult | Sputum - immunology | Benzamides - therapeutic use | Adult | Bronchitis - complications | Female | Benzamides - pharmacology | Eosinophils - pathology | Leukocyte Count | Receptors, CCR3 - antagonists & inhibitors | Asthma - physiopathology | Treatment Outcome | Bronchitis - physiopathology | Asthma - drug therapy | Methylurea Compounds - pharmacology | Methylurea Compounds - therapeutic use | Bronchitis - drug therapy | Pulmonary Eosinophilia - complications | Aged | Respiratory Function Tests | Chemotaxis, Leukocyte - immunology | Clinical trials | Bronchitis
Journal Article
American Journal of Pathology, The, ISSN 0002-9440, 2015, Volume 185, Issue 9, pp. 2534 - 2549
Choroidal neovascularization (CNV) is a defining feature of wet age-related macular degeneration. We examined the functional role of CCR3 in the development of...
Pathology | TARGET | SYSTEMIC ABSORPTION | MACULAR DEGENERATION | PATHOLOGY | VEGF-A | RANIBIZUMAB | EOTAXIN | DELIVERY | Wet Macular Degeneration - pathology | Mice, Inbred C57BL | Capillary Permeability - drug effects | Capillary Permeability - immunology | Vascular Endothelial Growth Factor A - metabolism | Animals | Wet Macular Degeneration - drug therapy | Choroidal Neovascularization - drug therapy | Choroidal Neovascularization - pathology | Angiogenesis Inhibitors - therapeutic use | Mice | Choroid - pathology | Disease Models, Animal | Receptors, CCR3 - antagonists & inhibitors | Regular
Pathology | TARGET | SYSTEMIC ABSORPTION | MACULAR DEGENERATION | PATHOLOGY | VEGF-A | RANIBIZUMAB | EOTAXIN | DELIVERY | Wet Macular Degeneration - pathology | Mice, Inbred C57BL | Capillary Permeability - drug effects | Capillary Permeability - immunology | Vascular Endothelial Growth Factor A - metabolism | Animals | Wet Macular Degeneration - drug therapy | Choroidal Neovascularization - drug therapy | Choroidal Neovascularization - pathology | Angiogenesis Inhibitors - therapeutic use | Mice | Choroid - pathology | Disease Models, Animal | Receptors, CCR3 - antagonists & inhibitors | Regular
Journal Article
The Journal of Allergy and Clinical Immunology, ISSN 0091-6749, 02/2019, Volume 143, Issue 2, pp. 552 - 553
biased antagonist | asthma | Allergic inflammation | eosinophil | inflammation | CCR3 | INHIBITION | ALLERGY | CHEMOKINE | IMMUNOLOGY | EOTAXIN
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 08/2000, Volume 275, Issue 34, pp. 25985 - 25992
We describe a small molecule chemokine receptor antagonist, UCB35625 (the trans-isomer J113863 published by Banyu Pharmaceutical Co., patent WO98/04554), which...
CHEMOATTRACTANT CYTOKINE | MESSENGER-RNA | CHEMOTACTIC CYTOKINES | BIOCHEMISTRY & MOLECULAR BIOLOGY | ENDOTHELIAL-CELLS | IN-VIVO | BONE-MARROW | CROSS-DESENSITIZATION | EOTAXIN RECEPTOR | MONOCLONAL-ANTIBODY | GUINEA-PIG MODEL | Chemokine CCL4 | HIV-1 - pathogenicity | Monocyte Chemoattractant Proteins - pharmacology | Chemokine CCL3 | Eosinophils - drug effects | Models, Chemical | Humans | Receptors, Chemokine - metabolism | Chemokine CCL11 | Chemokines, CC | Eosinophils - physiology | Animals | Drug Interactions | Flow Cytometry | Transfection | Mice | Receptors, CCR3 | Receptors, Chemokine - antagonists & inhibitors | Receptors, CCR1 | Receptors, Chemokine - drug effects | Cytokines - pharmacology | Xanthenes - pharmacology | Macrophage Inflammatory Proteins - pharmacology
CHEMOATTRACTANT CYTOKINE | MESSENGER-RNA | CHEMOTACTIC CYTOKINES | BIOCHEMISTRY & MOLECULAR BIOLOGY | ENDOTHELIAL-CELLS | IN-VIVO | BONE-MARROW | CROSS-DESENSITIZATION | EOTAXIN RECEPTOR | MONOCLONAL-ANTIBODY | GUINEA-PIG MODEL | Chemokine CCL4 | HIV-1 - pathogenicity | Monocyte Chemoattractant Proteins - pharmacology | Chemokine CCL3 | Eosinophils - drug effects | Models, Chemical | Humans | Receptors, Chemokine - metabolism | Chemokine CCL11 | Chemokines, CC | Eosinophils - physiology | Animals | Drug Interactions | Flow Cytometry | Transfection | Mice | Receptors, CCR3 | Receptors, Chemokine - antagonists & inhibitors | Receptors, CCR1 | Receptors, Chemokine - drug effects | Cytokines - pharmacology | Xanthenes - pharmacology | Macrophage Inflammatory Proteins - pharmacology
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2015, Volume 25, Issue 2, pp. 229 - 235
Rodent selectivity data of piperidine-4-yl-1 -indoles, a series of CC chemokine receptor-3 (CCR3) antagonists, are presented and discussed as part of an...
Chemokine | Receptor model | Piperidine-4-yl-1H-indoles | hERG | Rodent selectivity | CCR3 | Rodent selectivity hERG | CHEMISTRY, MEDICINAL | INHIBITION | CHEMISTRY, ORGANIC | MARAVIROC | DISCOVERY | Protein Structure, Tertiary | Piperidines - chemistry | Protein Structure, Secondary | Species Specificity | Piperidines - metabolism | Humans | Models, Molecular | Rats | Receptors, CCR3 - metabolism | Indoles - metabolism | Animals | Piperidines - pharmacology | Indoles - pharmacology | Mice | Indoles - chemistry | Receptors, CCR3 - antagonists & inhibitors | HERG
Chemokine | Receptor model | Piperidine-4-yl-1H-indoles | hERG | Rodent selectivity | CCR3 | Rodent selectivity hERG | CHEMISTRY, MEDICINAL | INHIBITION | CHEMISTRY, ORGANIC | MARAVIROC | DISCOVERY | Protein Structure, Tertiary | Piperidines - chemistry | Protein Structure, Secondary | Species Specificity | Piperidines - metabolism | Humans | Models, Molecular | Rats | Receptors, CCR3 - metabolism | Indoles - metabolism | Animals | Piperidines - pharmacology | Indoles - pharmacology | Mice | Indoles - chemistry | Receptors, CCR3 - antagonists & inhibitors | HERG
Journal Article
11.
Full Text
Recent progress in the development of antagonists to the chemokine receptors CCR3 and CCR4
Expert Opinion on Drug Discovery, ISSN 1746-0441, 05/2014, Volume 9, Issue 5, pp. 467 - 483
Introduction: The chemokine receptors CCR3 and CCR4 have been shown to be important therapeutic targets for the treatment of a variety of diseases. Although...
antagonists | chemokine | autoimmune | inflammation | asthma | CCR4 | CCR3 | Chemokine | Antagonists | Autoimmune | Inflammation | Asthma | INDAZOLE ARYLSULFONAMIDES | GENE-RELATED PEPTIDE | DIFFERENTIAL EXPRESSION | MACROPHAGE-DERIVED CHEMOKINE | INDUCED AIRWAY INFLAMMATION | CELLS IN-VITRO | MACULAR DEGENERATION | ACTIVATION-REGULATED CHEMOKINE | EPITHELIAL-CELLS | PHARMACOLOGY & PHARMACY | SMALL-MOLECULE ANTAGONISTS | Anti-Asthmatic Agents - pharmacology | Humans | Hypersensitivity, Immediate - drug therapy | Anti-Allergic Agents - pharmacology | Asthma - drug therapy | Receptors, CCR3 - antagonists & inhibitors | Receptors, CCR4 - antagonists & inhibitors
antagonists | chemokine | autoimmune | inflammation | asthma | CCR4 | CCR3 | Chemokine | Antagonists | Autoimmune | Inflammation | Asthma | INDAZOLE ARYLSULFONAMIDES | GENE-RELATED PEPTIDE | DIFFERENTIAL EXPRESSION | MACROPHAGE-DERIVED CHEMOKINE | INDUCED AIRWAY INFLAMMATION | CELLS IN-VITRO | MACULAR DEGENERATION | ACTIVATION-REGULATED CHEMOKINE | EPITHELIAL-CELLS | PHARMACOLOGY & PHARMACY | SMALL-MOLECULE ANTAGONISTS | Anti-Asthmatic Agents - pharmacology | Humans | Hypersensitivity, Immediate - drug therapy | Anti-Allergic Agents - pharmacology | Asthma - drug therapy | Receptors, CCR3 - antagonists & inhibitors | Receptors, CCR4 - antagonists & inhibitors
Journal Article
Journal of Natural Products, ISSN 0163-3864, 08/2016, Volume 79, Issue 8, pp. 2005 - 2013
CC chemokine receptor 3 (CCR3) is expressed selectively in eosinophils, basophils, and some Th2 cells and plays a major role in allergic diseases. A methanol...
ABSOLUTE-CONFIGURATION ASSIGNMENT | CHEMISTRY, MEDICINAL | ENANTIOSELECTIVE SYNTHESIS | ANTIALLERGIC ACTIVITIES | MACHILUS-THUNBERGII | EOSINOPHIL EOTAXIN RECEPTOR | PLANT SCIENCES | FUNCTIONAL LIGAND | NITRIC-OXIDE PRODUCTION | STELLARIA-DICHOTOMA | PHARMACOLOGY & PHARMACY | MOLECULAR-CLONING | BIOACTIVE CONSTITUENTS | Eosinophils - metabolism | Lignans - chemistry | Stereoisomerism | Furans - pharmacology | Humans | Myristica fragrans - chemistry | Molecular Structure | Chemotaxis - drug effects | Lignans - pharmacology | Lignans - isolation & purification | Receptors, CCR3 - antagonists & inhibitors
ABSOLUTE-CONFIGURATION ASSIGNMENT | CHEMISTRY, MEDICINAL | ENANTIOSELECTIVE SYNTHESIS | ANTIALLERGIC ACTIVITIES | MACHILUS-THUNBERGII | EOSINOPHIL EOTAXIN RECEPTOR | PLANT SCIENCES | FUNCTIONAL LIGAND | NITRIC-OXIDE PRODUCTION | STELLARIA-DICHOTOMA | PHARMACOLOGY & PHARMACY | MOLECULAR-CLONING | BIOACTIVE CONSTITUENTS | Eosinophils - metabolism | Lignans - chemistry | Stereoisomerism | Furans - pharmacology | Humans | Myristica fragrans - chemistry | Molecular Structure | Chemotaxis - drug effects | Lignans - pharmacology | Lignans - isolation & purification | Receptors, CCR3 - antagonists & inhibitors
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 08/2012, Volume 22, Issue 15, pp. 4951 - 4954
The synthesis and structure–activity relationships of ureas as CCR3 antagonists are described. Optimization starting with lead compound (IC = 190 nM) derived...
Urea derivatives | Allergic diseases | Proline moiety | CCR3 antagonists | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | ASTHMA | PART 1 | Naphthalenes - chemical synthesis | Naphthalenes - chemistry | Humans | Structure-Activity Relationship | Urea - chemical synthesis | Pyrrolidines - chemistry | Proline - chemistry | Receptors, CCR3 - metabolism | Pyrrolidines - chemical synthesis | Urea - analogs & derivatives | Pyrrolidines - metabolism | Protein Binding | Urea - metabolism | Drug Evaluation, Preclinical | Naphthalenes - metabolism | Receptors, CCR3 - antagonists & inhibitors | Urea
Urea derivatives | Allergic diseases | Proline moiety | CCR3 antagonists | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | ASTHMA | PART 1 | Naphthalenes - chemical synthesis | Naphthalenes - chemistry | Humans | Structure-Activity Relationship | Urea - chemical synthesis | Pyrrolidines - chemistry | Proline - chemistry | Receptors, CCR3 - metabolism | Pyrrolidines - chemical synthesis | Urea - analogs & derivatives | Pyrrolidines - metabolism | Protein Binding | Urea - metabolism | Drug Evaluation, Preclinical | Naphthalenes - metabolism | Receptors, CCR3 - antagonists & inhibitors | Urea
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 2008, Volume 16, Issue 1, pp. 144 - 156
The 6-fluoro-2-naphthylmethyl derivatives were prepared, and their inhibitory activities against CCR3 were evaluated. A novel class of potent CCR3 receptor...
6-fluoro-2-naphthylmethyl moiety | Allergic diseases | Nortropane derivatives | CCR3 antagonists | MURINE MODEL | CELLS | SELECTIVE ANTAGONIST | POTENT | CHEMISTRY, MEDICINAL | INFLAMMATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | CHEMOKINE RECEPTORS | EXPRESSION | EOTAXIN | DISCOVERY | Calcium - metabolism | Small Molecule Libraries | Humans | Inhibitory Concentration 50 | Chemokine CCL11 | Benzamides - pharmacology | Structure-Activity Relationship | Benzamides - chemical synthesis | Precursor Cells, B-Lymphoid | Receptors, CCR3 - antagonists & inhibitors
6-fluoro-2-naphthylmethyl moiety | Allergic diseases | Nortropane derivatives | CCR3 antagonists | MURINE MODEL | CELLS | SELECTIVE ANTAGONIST | POTENT | CHEMISTRY, MEDICINAL | INFLAMMATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | CHEMOKINE RECEPTORS | EXPRESSION | EOTAXIN | DISCOVERY | Calcium - metabolism | Small Molecule Libraries | Humans | Inhibitory Concentration 50 | Chemokine CCL11 | Benzamides - pharmacology | Structure-Activity Relationship | Benzamides - chemical synthesis | Precursor Cells, B-Lymphoid | Receptors, CCR3 - antagonists & inhibitors
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 12/2012, Volume 22, Issue 24, pp. 7702 - 7706
The discovery of potent small molecule dual antagonists of the human CCR3 and H receptors is described for the treatment of allergic diseases, for example,...
Chemokine antagonist | Receptor antagonist | Dual inhibitor | CCR3 | Allergic disease | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC
Chemokine antagonist | Receptor antagonist | Dual inhibitor | CCR3 | Allergic disease | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC
Journal Article