| Literature DB >> 21159507 |
Dale A Rudolph1, Curt A Dvorak, Lisa Dvorak, Diane Nepomuceno, Pascal Bonaventure, Timothy W Lovenberg, Nicholas I Carruthers.
Abstract
The synthesis and SAR for a novel series of tetrahydropyrido[3,2-c]pyrroles is described. Optimization of the pendant aryl ring lead to high binding affinity at the 5-HT(7) receptor when small lipophilic groups were placed in the para position. Modification of the N-benzyl group and secondary amine were not well tolerated. A representative set of compounds was shown to be functional antagonists of the 5-HT(7) receptor.Entities:
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Year: 2010 PMID： 21159507 DOI： 10.1016/j.bmcl.2010.11.078
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823