IACYLPIPERAZINE-2-(S)-[(N-AMINOALKYL)CARBOXAMIDES] AS NOVEL, POTENT SUBSTANCE-P RECEPTOR ANTAGONISTS

Authors
MILLS SG WU MT MACCOSS M BUDHU RJ DORN CP CASCIERI MA SADOWSKI S STRADER CD GREENLEE WJ
Citation
Sg. Mills et al., IACYLPIPERAZINE-2-(S)-[(N-AMINOALKYL)CARBOXAMIDES] AS NOVEL, POTENT SUBSTANCE-P RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 3(12), 1993, pp. 2707-2712
Citations number
19
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
12
Year of publication
1993
Pages
2707 - 2712
Database
ISI
SICI code
0960-894X(1993)3:12<2707:IANPS>2.0.ZU;2-B
Abstract
A series of N,N'-diacylpiperazine-2-carboxamides are shown to be antag onists of the NK-1 Substance P) receptor. Elaboration of the C2 sidech ain with aminoalkyl groups leads to two series of potent antagonists, one containing simple dialkylamino groups and the second featuring 2-m ethoxybenzylamino derivatives with divergent SARs with respect to subs titution at the C2 amide bond.