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3-羟基-4-芳基磺酰基四氢吡喃基-3-异羟肟酸是基质金属蛋白酶-13和软骨聚集蛋白聚糖酶的新型抑制剂。

3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.

作者信息

Noe Mark C, Snow Sheri L, Wolf-Gouveia Lilli A, Mitchell Peter G, Lopresti-Morrow Lori, Reeves Lisa M, Yocum Sue A, Liras Jennifer L, Vaughn Marcie

机构信息

Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA.

出版信息

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4727-30. doi: 10.1016/j.bmcl.2004.06.081.

DOI:10.1016/j.bmcl.2004.06.081
PMID:15324896
Abstract

N-Hydroxy-3-hydroxy-4-arylsulfonyltetrahydropyranyl-3-carboxamides were designed as novel inhibitors of MMP-13 and aggrecanase based on known endocyclic hydroxamate inhibitors of matrix metalloproteinases. These compounds offer favorable physicochemical properties and low metabolic clearance. Synthesis and structure-activity relationships are reported.

摘要

基于已知的基质金属蛋白酶内酰胺类羟肟酸抑制剂，设计了N-羟基-3-羟基-4-芳基磺酰基四氢吡喃基-3-羧酰胺作为MMP-13和聚集蛋白聚糖酶的新型抑制剂。这些化合物具有良好的物理化学性质和低代谢清除率。本文报道了其合成及构效关系。

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