186602-56-2Relevant articles and documents
INHIBITORS OF METALLOPROTEASES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME AND METHODS OF THEIR USE
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, (2008/06/13)
Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
Malonyl α-mercaptoketones and α-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors
Campbell, David A.,Xiao, Xiao-Yi,Harris, David,Ida, Satoru,Mortezaei, Reza,Ngu, Khehyong,Shi, Lihong,Tien, David,Wang, Yongwen,Navre, Marc,Patel, Dinesh V.,Sharr, Michele A.,DiJoseph, John F.,Killar, Loran M.,Leone, Christina L.,Levin, Jeremy I.,Skotnicki, Jerauld S.
, p. 1157 - 1162 (2007/10/03)
A novel series of matrix metalloproteinase (MMP) inhibitors is described. Incorporation of a terminal α-mercaptoketone or α- mercaptoalcohol in the zinc binding domain of a series of inhibitors led to compounds exhibiting low nanomolar activity against collagenase-1 (MMP-1), stromelysin (MMP-3), and gelatinase-B (MMP-9).