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J Med Chem. 2009 Aug 13;52(15):4955-9. doi: 10.1021/jm900374r.

Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.

Author information

1
Chemical Sciences, Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA. zhoud@wyeth.com

Abstract

On the basis of the previously reported clinical candidate, SSA-426 (1), a series of related 2-piperazin-1-ylquinoline derivatives 3-16 were synthesized and evaluated as dual-acting serotonin (5-HT) reuptake inhibitors and 5-HT1A receptor antagonists. In particular, compound 7 exhibits potent functional activities at both the 5-HT transporter and 5-HT1A receptor, good selectivity over the alpha1-adrenergic and dopaminergic receptors, acceptable pharmacokinetic properties, and a favorable in vivo profile.

PMID:
19719241
DOI:
10.1021/jm900374r
[Indexed for MEDLINE]

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