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Bioorg Med Chem Lett. 2011 Jan 1;21(1):42-4. doi: 10.1016/j.bmcl.2010.11.078. Epub 2010 Nov 24.

Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT(7) antagonists.

Author information

1
Johnson & Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, United States. drudolph@its.jnj.com

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.

PMID:
21159507
DOI:
10.1016/j.bmcl.2010.11.078
[Indexed for MEDLINE]

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