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Bioorg Med Chem Lett. 2010 Sep 1;20(17):5286-9. doi: 10.1016/j.bmcl.2010.06.134. Epub 2010 Jul 1.

Biaryl substituted hydantoin compounds as TACE inhibitors.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, USA. wensheng.yu@merck.com

Abstract

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.

PMID:
20663669
DOI:
10.1016/j.bmcl.2010.06.134
[Indexed for MEDLINE]

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