MMP-13 选择性 α-砜羟酰胺：选择性 P1' 酰胺的鉴定。
MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides.
机构信息
Department of Medicinal Chemistry, Pfizer Research & Development, 700 Chesterfield Village Parkway, St. Louis, MO 63198, USA.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):2823-5. doi: 10.1016/j.bmcl.2011.03.095. Epub 2011 Apr 1.
PMID:21493063
Abstract
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we report on a series of hydroxamic acids with a flexible amide P1' substituents. We identify an amide which spares both MMP-1 and -14, and shows >500 fold selectivity for MMP-13 versus MMP-2 and -8.
摘要
延续我们设计优先对 MMP-13 具有高效力和选择性的化合物的兴趣，我们报告了一系列具有柔性酰胺 P1'取代基的羟肟酸。我们确定了一种酰胺，它对 MMP-1 和 -14 均无抑制作用，并且对 MMP-13 相对于 MMP-2 和 -8 的选择性超过 500 倍。
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