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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.

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Pyridine derivatives R 0380 Lactams as Prostanoid Receptor Ligands. Part 4. 2-Piperidones as Selective EP 4 Receptor Agonists. -Compounds (VI) and (VIII) are reported to show the strongest target receptor-binding activity of all tested compounds. -(ELWORTHY*, T. R.; BRILL, E. R.; CAIRES, C. C.; KIM, W.; LACH, L. K.; TRACY, J. L.; CHIOU, S.-S.; Bioorg. Med. Chem. Lett. 15 (2005) 10, 2523-2526; Dep. Med. Chem., Roche Biosci., Palo Alto, CA 94304, USA; Eng.) -C. Oppel 38-150

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