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Discovery of new C3aR ligands. Part 1: Arginine derivatives
The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflammation after aerosol administration.
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| Published in: | Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3258-3261 |
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| Main Authors: | , , , , , , , , , , , , , , , , |
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| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c415t-5932d1965be9be88c5f4701397870a71f0c24da5e2d04719b6c5e32eb5cb91953 |
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| cites | cdi_FETCH-LOGICAL-c415t-5932d1965be9be88c5f4701397870a71f0c24da5e2d04719b6c5e32eb5cb91953 |
| container_end_page | 3261 |
| container_issue | 12 |
| container_start_page | 3258 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 17 |
| creator | Denonne, Frédéric Binet, Sophie Burton, Maggi Collart, Philippe Dipesa, Alan Ganguly, Tanmoy Giannaras, Alexander Kumar, Seema Lewis, Timothy Maounis, Florence Nicolas, Jean-Marie Mansley, Tamsin Pasau, Patrick Preda, Dorin Stebbins, Karin Volosov, Alexander Zou, Dong |
| description | The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflammation after aerosol administration. |
| doi_str_mv | 10.1016/j.bmcl.2007.04.022 |
| format | article |
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| ispartof | Bioorganic & medicinal chemistry letters, 2007-06, Vol.17 (12), p.3258-3261 |
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| language | eng |
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| source | Elsevier:Jisc Collections:Elsevier Read and Publish Agreement 2022-2024:Freedom Collection (Reading list) |
| subjects | Aerosols - administration & dosage Animals Arginine Arginine - analogs & derivatives Arginine - chemical synthesis Arginine - pharmacology Biological and medical sciences C3a Complement Activation - drug effects Inflammation Inflammation - chemically induced Inflammation - pathology Ligands Medical sciences Membrane Proteins - metabolism Mice Mice, Inbred BALB C Models, Biological Pharmacology. Drug treatments Protein Binding Protein-Serine-Threonine Kinases - metabolism Receptors, Complement - metabolism Respiratory Mucosa - pathology Respiratory system Structure-Activity Relationship Time Factors |
| title | Discovery of new C3aR ligands. Part 1: Arginine derivatives |
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