- 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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- 2,4- and 2,5-disubstituted arylthiazoles: Rapid synthesis by C-H coupling and biological evaluation
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Life-threatening infections caused by bacteria that have developed resistance to common antibiotics, such as methicillin-resistant Staphylococcus aureus (MRSA), have become a serious problem in hospitals and other areas all over the world. Thus, the development of an effective class of antibiotics against these bacteria is an urgent subject. Herein, we report a step-economical and diversity-oriented synthesis of a series of 2-arylidenehydrazinyl-4- arylthiazole and 2-arylidenehydrazinyl-5-arylthiazole analogues that utilizes C-H coupling methodologies. A library of 54 new congeners were synthesized and tested for their biological potential. Moreover, new knowledge regarding the structure-activity relationships (SARs) of these heterobiaryl compounds was collected. Copyright
- Lohrey, Lilia,Uehara, Takahiro N.,Tani, Satoshi,Yamaguchi, Junichiro,Humpf, Hans-Ulrich,Itami, Kenichiro
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supporting information
p. 3387 - 3394
(2014/06/09)
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- Spectrophotometric and polarographic studies on the kinetics of hydrolysis of N-(6-methyl-5-nitropyridin-2-yl methylidene)-N′-(substituted thiazol-2-yl)hydrazines
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The kinetics of the hydrolysis of hydrazpne derived from nitropyridine 2-carboxaldehyde and 2-hydrazino-4-substituted thiazoles la-e in 10% (v/v) DMF-buffer mixture has been investigated by applying two independent and different techniques viz UV-spectrop
- El-Nady, Abobakr M.
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p. 1081 - 1086
(2007/10/03)
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- MAOI activity of some novel series of substituted thiazol-2-yl-hydrazines
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Three series of 2-thiazolylhydrazines were synthetized and evaluated for their MAO inhibitory (MAOI) activity, both by in vivo tests, to assay their influence on several MAOI activity-related parameters (the variation on blood pressure induced by tyramine
- Mazzone,Pignatello,Panico,Mazzone,Puglisi,Pennisi,Raciti,Mazzone,Matera
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p. 902 - 910
(2007/10/02)
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