- Cardioprotective effect of novel sulphonamides-1,3,5-triazine conjugates against ischaemic–reperfusion injury via selective inhibition of MMP-9
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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.
- Zheng, Xiao-Zhu,Zhou, Jia-Li,Ye, Jing,Guo, Pei-Pei,Lin, Chun-Shui
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- Synthesis of imidazolinones, azetidinones and formazans from hydrazino-s-triazines as potential antimicrobial agents
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2,4-Bis(ethylamino)-6-hydrazino-s-triazine (1) on treatment with 4-arylidene-2-phenyl-5-oxazolinone gives 4-arylidene-1--2-phenyl-5-oxo-2-imidazolines (2a-j).Also, compound 1 when refluxed with aromatic aldehydes yield the corresponding hydrazones (3a-j) which on reaction with chloroacetyl chloride and Et3N in dioxane afford 4-aryl-1--3-chloro-2-azetidinones (4a-j).The hydrazones (3a-j) also react with sulphanilamides furnishing 2,4-bis(ethylamino)-6--s-triazines (5a-j).Compounds 2d-q, 2i, 3a-c, 3e-f, 4a-g and 4i exhibit highest antimicrobial activity against the various strains of bacteria and fungi.
- Joshi, Nailesh,Bapodra, Atul,Parekh, Hansa
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p. 662 - 665
(2007/10/02)
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