A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist
A recently reported dual LPA(1)/LPA(3) receptor antagonist (1) has been modified so as to modulate the basicity, sterics, and dipole moment of the 2-pyridyl moiety. Additionally, the implications of installing nonhydrolyzable phosphate head group isosteres with regard to antagonist potency and selec...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2004-08, Vol.14 (15), p.4069-4074 |
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| container_end_page | 4074 |
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| container_issue | 15 |
| container_start_page | 4069 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 14 |
| creator | Heasley, Brian H Jarosz, Renata Carter, Karen M Van, S Jenny Lynch, Kevin R Macdonald, Timothy L |
| description | A recently reported dual LPA(1)/LPA(3) receptor antagonist (1) has been modified so as to modulate the basicity, sterics, and dipole moment of the 2-pyridyl moiety. Additionally, the implications of installing nonhydrolyzable phosphate head group isosteres with regard to antagonist potency and selectivity at LPA receptors is described. This study has resulted in the development of the first nonhydrolyzable and presumably phosphatase-resistant LPA(3)-selective antagonist reported to date. |
| doi_str_mv | 10.1016/j.bmcl.2004.05.023 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2004-08, Vol.14 (15), p.4069-4074 |
| issn | 0960-894X |
| language | eng |
| recordid | cdi_proquest_miscellaneous_66664186 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Fibroblasts - drug effects Fibroblasts - physiology Guanosine 5'-O-(3-Thiotriphosphate) - metabolism Molecular Conformation Molecular Structure Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Receptors, Lysophosphatidic Acid - antagonists & inhibitors Structure-Activity Relationship |
| title | A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist |
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