- Novel thiazole–pyrazolone hybrids as potent ACE inhibitors and their cardioprotective effect on isoproterenol-induced myocardial infarction
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A facile synthesis of a group of novel thiazole–pyrazolone hybrids and their investigation for angiotensin-converting enzyme (ACE) inhibition are reported in this study. These compounds were synthesized using a well-known approach, based on the condensation of ethyl acetoacetate with thiazolylhydrazines, and characterized by various spectroscopic and analytical techniques. The entire set of compounds displayed a moderate-to-excellent inhibitory activity against ACE. In particular, compound 4i was found to be the most potent ACE inhibitor and was further studied for cardioprotective effects against isoproterenol (ISO)-induced myocardial infarction (MI) in rats. Compound 4i improved the cardiac function and prevented cardiac injury induced by ISO in Sprague Dawley rats. The levels of oxidative stress and proinflammatory cytokines were also restored to near normal by 4i as compared with the ISO group. In the Western blot analysis, compound 4i prevented mitochondrial apoptosis after MI by downregulating the expression of cleaved caspase-3 and Bax, with the upregulation of Bcl-2, as compared with the ISO group.
- You, Hongwen,Su, Xinyou,Su, Guoying
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- SYNTHESIS AND PROPERTIES OF 1,3,4-THIADIAZINE DERIVATIVES. 1. INVESTIGATION OF THE CONDENSATION OF SUBSTITUTED PHENACYL BROMIDES AND BROMOACETYLPYRIDINES WITH THIOSEMICARBAZIDE
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2-Amino-5-aryl(pyridyl)-6H-1,3,4-thiadiazines and isomeric 2-hydrazino-4-aryl(pyridyl)thiazoles, the ration of which depends on the reaction conditions, were obtained by the reaction of substituted phenacyl bromides and bromoacetylpyridines with thiosemicarbazide.
- Novikova, A. P.,Perova, N. M.,Egorova, L. G.,Bragina, E. I.
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p. 666 - 668
(2007/10/02)
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