| 11714604 |
Shaw D, Chicchi GG, Elliott JM, Kurtz M, Morrison D, Ridgill MP, Szeto N, Watt AP, Williams AR, Swain CJ: 2-Aryl indole NK (1) antagonists: optimisation of the amide substituent. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3031-4.
The in vivo properties of a series of 2-arylindole NK (1) 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. |
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