Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors

Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors
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DOI:
10.1016/j.bmcl.2008.12.053
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发表时间:
2009-02-01
影响因子:
2.7
通讯作者:
Oballa, Renata M.
Oballa, Renata M.
中科院分区:
医学4区
文献类型:
--
作者:
Boyd, Michael J.;Crane, Sheldon N.;Oballa, Renata M.

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氨基酮弹头被探索作为一个有效的和选择性的组织蛋白酶K抑制剂的腈基团的替代品。所得到的化合物是有效的和选择性的组织蛋白酶K抑制剂,这些腈替代品对代谢和药代动力学有显著的影响。(c) 2008 Elsevier Ltd.版权所有。
Amino ketone warheads were explored as alternatives to the nitrile group of a potent and selective cathepsin K inhibitor. The resulting compounds were potent and selective inhibitors of cathepsin K and these nitrile replacements had a significant effect on metabolism and pharmacokinetics. (c) 2008 Elsevier Ltd. All rights reserved.