Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.

Bioorg Med Chem Lett

Departments of Medicinal Chemistry and Pharmacology, Pfizer Research & Development, 4901 Searle Parkway, Skokie, IL 60077, USA.

Published: November 2004

Azaadamantanone 1 was converted to a series of aminoazaadamantane benzamides 9a-d, which were profiled for serotonin receptor activity. Aminomethylazaadamantane SC-54750 is a potent 5-HT(4) agonist and 5-HT(3) antagonist with in vivo efficacy in gastroparesis models and also inhibits cisplatin-induced emesis.

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http://dx.doi.org/10.1016/j.bmcl.2004.09.005DOI Listing

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