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Chem Biol Drug Des. 2016 Nov;88(5):756-765. doi: 10.1111/cbdd.12807. Epub 2016 Jul 15.

Cardioprotective effect of novel sulphonamides-1,3,5-triazine conjugates against ischaemic-reperfusion injury via selective inhibition of MMP-9.

Author information

1
Department of Anesthesiology, Zhejiang Hospital, Hangzhou, Zhejiang, China.
2
Department of Anesthesiology, Nanfang Hospital of Southern Medical University, Guangzhou, Guangdong, China.
3
Department of Anesthesiology, Nanfang Hospital of Southern Medical University, Guangzhou, Guangdong, China. linchunshui@hotmail.com.

Abstract

Diseases affecting cardiovascular system are ranked as a top most cause of morbidity and mortality. Herein, a novel class sulphonamides-1,3,5-triazine conjugates have been synthesized and tested for inhibitory activity against MMP-2 and MMP-9. The results of the study showed that these molecules efficiently inhibit MMP-9 than MMP-2, revealing compound 8e as the most potent inhibitor (IC50  = 2.34 ± 0.56 nm). Due to involvement of MMP-9 in many cardiovascular diseases, particularly in myocardial ischaemia (MI), compound 8e was further subjected for the determination of the protective effect on isoproterenol (ISO)-induced myocardial injury in rats.

KEYWORDS:

1,3,5-triazine; MMP inhibition; biochemical assay; myocardial ischaemia; sulphonamide

PMID:
27317634
DOI:
10.1111/cbdd.12807
[Indexed for MEDLINE]

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