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Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent

Authors :
Penny G. Threlkeld
Nixon James Arthur
Carl L. McMillian
Bruce D. Gitter
Stephen W. Kaldor
Karen Lynn Lobb
Philip Arthur Hipskind
James E. Fritz
Source :
Bioorganicmedicinal chemistry letters. 11(13)
Publication Year :
2001

Abstract

Solution-phase, parallel-synthesis techniques were used to optimize a series of nonbasic NK-1 antagonists, resulting in the identification of (R)-26, an orally bioavailable compound with subnanomolar potency.

Details

ISSN :
0960894X
Volume :
11
Issue :
13
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry letters
Accession number :
edsair.doi.dedup.....258988fc8ccce683184646225a6fbc5d