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首页> 外文期刊>Journal of Medicinal Chemistry >Synthesis and Structure-Activity Relationship of α-Sulfonylhydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis
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Synthesis and Structure-Activity Relationship of α-Sulfonylhydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis

机译：新型口服活性基质金属蛋白酶抑制剂α-磺酰基异羟肟酸的合成及其构效关系

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摘要

The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue degradation. These enzymes are strictly regulated by endogenous inhibitors such as tissue inhibitors of MMPs and α_2-macroglobulins. Overexpression of these enzymes has been implicated in various pathological disorders such as arthritis, tumor metastasis, cardiovascular diseases, and multiple sclerosis. Developing effective small-molecule inhibitors to modulate MMP activity is one approach to treat these degenerative diseases. The present work focuses on the discovery and SAR of novel N-hydroxy-α-phenylsulfonylacetamide derivatives, which are potent, selective, and orally active MMP inhibitors.
机译：基质金属蛋白酶（MMP）是一族含锌内肽酶，在生理和病理组织降解中均起关键作用。这些酶受到内源性抑制剂（例如MMPs和α_2-巨球蛋白的组织抑制剂）的严格调控。这些酶的过表达与多种病理疾病有关，例如关节炎，肿瘤转移，心血管疾病和多发性硬化。开发有效的小分子抑制剂来调节MMP活性是治疗这些退行性疾病的一种方法。目前的工作集中在新型N-羟基-α-苯基磺酰基乙酰胺衍生物的发现和SAR上，它们是有效，选择性和口服活性的MMP抑制剂。

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