| Autor: |
Elworthy TR; Roche Palo Alto, California 94304, USA. todd.elworthy@Roche.com, Brill ER, Chiou SS, Chu F, Harris JR, Hendricks RT, Huang J, Kim W, Lach LK, Mirzadegan T, Yee C, Walker KA |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2004 Dec 02; Vol. 47 (25), pp. 6124-7. |
| DOI: |
10.1021/jm049290a |
| Abstrakt: |
Two distinct synthetic schemes were applied to access heteroatom-containing alpha-chain lactams or lactams terminated as aryl acids. The latter lactams were devised using a pharmacophore for EP(4) receptor activity. gamma-Lactams were characterized for their prostanoid EP receptor affinities and EP(4) activity and found to be selective for the EP(2) and EP(4) receptors or selective for the EP(4) subtype. Benzoic acid 17 displayed enhanced in vivo exposure relative to 3. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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