Volume 353, Issue 12 2000140

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Novel thiazole–pyrazolone hybrids as potent ACE inhibitors and their cardioprotective effect on isoproterenol-induced myocardial infarction

Hongwen You

Department of Cardiology, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Jinan, Shandong, China

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Xinyou Su,

Xinyou Su

Department of Oncology, Jinan Central Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, China

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Guoying Su,

Corresponding Author

Guoying Su

[email protected]

orcid.org/0000-0002-4462-2587

Department of Cardiology, Jinan Central Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, China

Correspondence Guoying Su, Department of Cardiology, Jinan Central Hospital, Cheeloo College of Medicine, Shandong University, Jinan, 250013 Shandong, China.

Email: [email protected]

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Hongwen You,

Hongwen You

Department of Cardiology, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Jinan, Shandong, China

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Xinyou Su,

Xinyou Su

Department of Oncology, Jinan Central Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, China

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Guoying Su,

Corresponding Author

Guoying Su

[email protected]

orcid.org/0000-0002-4462-2587

Department of Cardiology, Jinan Central Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, China

Correspondence Guoying Su, Department of Cardiology, Jinan Central Hospital, Cheeloo College of Medicine, Shandong University, Jinan, 250013 Shandong, China.

Email: [email protected]

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First published: 25 August 2020

https://doi.org/10.1002/ardp.202000140

Citations: 6

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Abstract

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.

CONFLICTS OF INTERESTS

The authors declare that there are no conflicts of interests.

Open Research

DATA AVAILABILITY STATEMENT

The data that support the findings of this study are available from the corresponding author upon reasonable request.

Supporting Information

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Volume353, Issue12

December 2020

2000140

Novel thiazole–pyrazolone hybrids as potent ACE inhibitors and their cardioprotective effect on isoproterenol-induced myocardial infarction

Abstract

CONFLICTS OF INTERESTS

Open Research

DATA AVAILABILITY STATEMENT

Supporting Information

REFERENCES

Citing Literature

References

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Novel thiazole–pyrazolone hybrids as potent ACE inhibitors and their cardioprotective effect on isoproterenol-induced myocardial infarction

Abstract

CONFLICTS OF INTERESTS

Open Research

DATA AVAILABILITY STATEMENT

Supporting Information

REFERENCES

Citing Literature

References

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