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

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (1), p.42-44
Hauptverfasser:	Rudolph, Dale A, Dvorak, Curt A, Dvorak, Lisa, Nepomuceno, Diane, Bonaventure, Pascal, Lovenberg, Timothy W, Carruthers, Nicholas I
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Protein Binding Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacokinetics Rats Receptors, Serotonin - chemistry Receptors, Serotonin - metabolism Serotonin Antagonists - chemical synthesis Serotonin Antagonists - chemistry Serotonin Antagonists - pharmacokinetics Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2010.11.078