[摘要]：We disclose further optimization of hydantoin TNF-alpha convertase enzyme (TACE) inhibitors. SAR with respect to the non-prime region of TACE active site was explored. A series of biaryl substituted hydantoin compounds was shown to have sub-nanomolar K-i, good rat PK, and good selectivity versus MMP-1, -2, -3, -7, -9, and -13. (C) 2010 Published by Elsevier Ltd.
