Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping
We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2008-04, Vol.18 (8), p.2684-2690 |
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| container_end_page | 2690 |
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| container_issue | 8 |
| container_start_page | 2684 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 18 |
| creator | HALL, Adrian BILLINTON, Andy THEOBALD, Pamela J BROWN, Susan H CHOWDHURY, Anita GIBLIN, Gerard M. P GOLDSMITH, Paul HURST, David N NAYLOR, Alan PATEL, Sadhana SCOCCITTI, Tiziana |
| description | We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain. |
| doi_str_mv | 10.1016/j.bmcl.2008.03.018 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2008-04, Vol.18 (8), p.2684-2690 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_69103839 |
| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Analgesics Animals Biological and medical sciences Humans Hydrogen Bonding Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Medical sciences Microsomes, Liver - drug effects Microsomes, Liver - metabolism Models, Molecular Molecular Structure Neuropharmacology Pharmacology. Drug treatments Rats Receptors, Prostaglandin E - antagonists & inhibitors Receptors, Prostaglandin E - metabolism Receptors, Prostaglandin E, EP1 Subtype Structure-Activity Relationship Thiazoles - chemistry |
| title | Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping |
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