Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamides
摘要:
A series of meso-amino(methyl)azanoradamantane benzamides has been prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis mucosae (TMM) assay. Compound 8i is the most potent 5-HT4 agonist in the series, with an EC50 of 217 nM. (C) 1997 Elsevier Science Ltd.
[EN] MUSCARINIC AGONISTS AND ANTAGONISTS<br/>[FR] AGONISTES ET ANTAGONISTES MUSCARINIQUES
申请人:UCB SA
公开号:WO2000011001A1
公开(公告)日:2000-03-02
The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.
The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.
Effect of Remote Substitution on Face Selection in Addition Reactions of Nor- and Homoadamantan-9-ones and of Several Analogues
作者:Mira Kaselj、Elena M. Gonikberg、William J. le Noble
DOI:10.1021/jo9718197
日期:1998.5.1
The effects of 3-halo substitution on face selection in borohydride reductions of both nor-and homoadamantan-9-ones l-X and 3-X. respectively, have been compared with those of 5-halo substitution in the parent 5-haloadamantan-2-ones 2-X, The differences between the product ratios in these three compounds are small, but the selectivity of 2-X is somewhat larger than that of either of the homologues. This is also true of the corresponding aza-and diazaadamantanones, and of an electrophilic addition. It is concluded that the approach angle of the reagent is not a sensitive variable in addition reactions of cyclohexanone and its derivatives, and that well-aligned antiperiplanar bonds are preferred to achieve maximal remote substituent induced selectivities.