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N-Substituted dibenzoxazepines as analgesic PGE2 antagonists

✍ Scribed by Hallinan, E. Ann.; Hagen, Timothy J.; Husa, Robert K.; Tsymbalov, Sofya; Rao, Shashidhar N.; vanHoeck, Jean Pierre; Rafferty, Michael F.; Stapelfeld, Awilda; Savage, Michael A.; Reichman, Melvin


Book ID
127321642
Publisher
American Chemical Society
Year
1993
Tongue
English
Weight
936 KB
Volume
36
Category
Article
ISSN
0022-2623

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The identification of substituted benzot
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We disclose herein our preliminary SAR study on the identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists. A potent EP(4) antagonist 6a (K(i)=1.4nM with 10% HSA) was identified. Furthermore, we found that an acidic group was not essential for the EP(4) ant