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Bioorg Med Chem Lett. 2003 Feb 10;13(3):437-42.

Discovery of orally bioavailable NK1 receptor antagonists.

Author information

1
Chemistry Department, UCB Pharma, Chemin du Foriest, B-1420, Braine-l'Alleud, Belgium. christophe.genicot@ucb-group.com

Abstract

Benzyloxyphenethylpiperazines are a new class of high affinity NK1 receptor antagonists. Oral bioavailability and selectivity can be fine tuned by the nature of the substituents on the basic nitrogen atom. Addition of substituents with a carboxylic acid group led to very selective and orally active NK1 antagonists free of interaction with L-type calcium channels.

PMID:
12565946
DOI:
10.1016/s0960-894x(02)00956-3
[Indexed for MEDLINE]

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