Tricyclic aminopyrimidine histamine H sub(4 receptor antagonists)
This report discloses the development of a series of tricyclic histamine H sub(4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and wate...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (21), p.6577-6581 |
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| Sprache: | eng |
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| container_end_page | 6581 |
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| container_issue | 21 |
| container_start_page | 6577 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 21 |
| creator | Savall, Brad M Gomez, Laurent Chavez, Frank Curtis, Michael Meduna, Steven P Kearney, Aaron Dunford, Paul Cowden, Jeffery Thurmond, Robin L Grice, Cheryl Edwards, James P |
| description | This report discloses the development of a series of tricyclic histamine H sub(4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H) sub(4) receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model. |
| doi_str_mv | 10.1016/j.bmcl.2011.08.014 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6577-6581 |
| issn | 0960-894X |
| language | eng |
| recordid | cdi_proquest_miscellaneous_904499074 |
| source | ScienceDirect Journals (5 years ago - present) |
| title | Tricyclic aminopyrimidine histamine H sub(4 receptor antagonists) |
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