Antinociceptive (aminoalkyl) indoles

…, TE D'Ambra, V Kumar, MA Eissenstat…

文献索引：Bell, Malcolm R.; D'Ambra, Thomas E.; Kumar, Virendra; Eissenstat, Michael A.; Herrmann, John L.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1099 - 1110

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被引用次数: 161

摘要

The (aminoa1kyl) indole (AAI) derivative pravadoline (la) inhibited prostaglandin (PG) synthesis in mouse brain microsomes in vitro and ex vivo and exhibited antinociceptive activity in several rodent assays. In vitro structure-activity relationship studies of this new class of PG synthesis inhibitors revealed a correspondence in three respects to those reported for the arylacetic acids:(1)“a-methylation” caused an increase in PG inhibitory ...