1.
Bioorg Med Chem Lett
; 22(4): 1606-10, 2012 Feb 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22264487
RESUMO
Tropanylamide was investigated as a possible scaffold for ß-tryptase inhibitors with a basic benzylamine P1 group and a substituted thiophene P4 group. Comparing to piperidinylamide, the tropanylamide scaffold is much more rigid, which presents less opportunity for the inhibitor to bind with off-target proteins, such as cytochrome P450, SSAO, and hERG potassium channel. The proposed binding mode was further confirmed by an in-house X-ray structure through co-crystallization.