Title of article
2-Aryl indole NK1 antagonists: optimisation of the amide substituent
Author/Authors
Duncan Shaw، نويسنده , , Gary G. Chicchi، نويسنده , , Jason M. Elliott، نويسنده , , Marc Kurtz، نويسنده , , Denise Morrison، نويسنده , , Mark P. Ridgill، نويسنده , , Nicola Szeto، نويسنده , , Alan P. Watt، نويسنده , , Angela R. Williams، نويسنده , , Christopher J. Swain، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
4
From page
3031
To page
3034
Abstract
The in vivo properties of a series of 2-arylindole NK1 antagonists have been improved, by modification of the amide substituent. The 1-(2-methoxyphenyl)piperazine amide was identified as a major area of metabolism in the lead compound 1. Replacement of this amine moiety by a 4-benzyl-4-hydroxypiperidine resulted in a compound 18 with reduced clearance and improved central duration of action.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791786
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