Design, Synthesis, and Pharmacological Activity of a New Matrix Metalloproteinase-9 Inhibitor

被引：1

作者：

Grigorkevich, O. S. ^{[1
]}

Mokrov, G. V. ^{[1
]}

Dyabina, A. S. ^{[1
]}

Stolyaruk, V. N. ^{[1
]}

Tsorin, I. B. ^{[1
]}

Ionova, E. O. ^{[1
]}

Kryzhanovskii, S. A. ^{[1
]}

Gudasheva, T. A. ^{[1
]}

Durnev, A. D. ^{[1
]}

机构：

[1] VV Zakusov Sci Res Inst Pharmacol, 8 Baltiiskaya St, Moscow 125315, Russia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2018年 / 52卷 / 01期

关键词：

matrix metalloproteinases; gelatinase B; MMP-9; inhibitors; benzoylamino(phenylsulfonyl)amino acids; cardioprotective substances; early postinfarct myocardial remodeling; MATRIX-METALLOPROTEINASE; MYOCARDIAL-INFARCTION; MMP INHIBITORS; TISSUE INHIBITOR; AMIDE SYNTHESIS; SELECTIVITY; COMPLEXES; DOCKING; GLIDE; TRIAL;

D O I：

10.1007/s11094-018-1761-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The new MMP-9 inhibitor 1-{4-[(4-chlorobenzoyl)amino]phenyl}sulfonyl-L-proline, with a theoretical inhibition constant of IC50 = 4 x 10(5) M, was constructed on the basis of structural requirements for selective inhibitors of gelatinases. This constructed compound and its close structural analogs were synthesized and these substances were found to have low toxicity, (LD50 > 300 mg/kg). The new inhibitor given p.o. at a dose of 20 mg/kg/day on the background of acute myocardial infarction significantly decreased the content of immunoreactive MMP-9 in plasma in rats, to the level obtained with doxycycline.

引用

页码：30 / 36

页数：7

共 36 条

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