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2-(6'-甲氧基-3',4'-二氢-1'-萘基)-4H-3,1-苯并恶嗪-4-酮作为人白细胞弹性蛋白酶新型强效底物抑制剂的合成、体外及体内评价

Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.

作者信息

Arcadi A, Asti C, Brandolini L, Caselli G, Marinelli F, Ruggieri V

机构信息

Dipartimento di Chimica, Ingegneria Chimica e Materiali, Università degli Studi di L'Aquila, Italy.

出版信息

Bioorg Med Chem Lett. 1999 May 3;9(9):1291-4. doi: 10.1016/s0960-894x(99)00168-7.

Abstract

The title 2-vinyl-4H-3,1-benzoxazin-4-one has been synthesised and tested for inhibitory activity against human leukocyte elastase. The compound has shown activity both in vitro towards human sputum elastase and in vivo in an hemorrhagic assay.

摘要

已合成了标题化合物2-乙烯基-4H-3,1-苯并恶嗪-4-酮,并测试了其对人白细胞弹性蛋白酶的抑制活性。该化合物在体外对人痰液弹性蛋白酶以及在体内出血试验中均显示出活性。

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