G. R. Ott, N. Asakawa, Rui-Qin Liu
Feb 15, 2008
Citations
0
Influential Citations
15
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
Two novel oxaspiro[4.4]nonane beta-benzamido hydroxamic scaffolds have been synthesized in enantio- and diasteriomerically pure form. These templates proved to be exceptional platforms that have led to the discovery of potent inhibitors of TACE that are active in a cellular assay measuring suppression of LPS-induced TNF-alpha. Furthermore, these inhibitors are selective against related MMPs, demonstrate permeability in a Caco-2 assay, and display good oral bioavailability.