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The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.
Authors:J I Levin  J M Chen  M T Du  F C Nelson  T Wehr  J F DiJoseph  L M Killar  S Skala  A Sung  M A Sharr  C E Roth  G Jin  R Cowling  L Di  M Sherman  Z B Xu  C J March  K M Mohler  R A Black  J S Skotnicki
Institution:Wyeth-Ayerst Research, 401N. Middletown Rd., Pearl River, NY 10965, USA. levinji@war.wyeth.com
Abstract:Anthranilic acid derivatives bearing basic amines were prepared and evaluated in vitro and in vivo as inhibitors of MMP-1, MMP-9, MMP-13, and TACE. Piperazine 4u has been identified as a potent, selective, orally active inhibitor of MMP-9 and MMP-13.
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