Development and Structural Modifications of Rupestonic Acid Derivatives as Novel Anti‐Influenza Agents: A Mini Review of The Last 10 Years

Yumaier, Abulimiti; Cui, Zhi‐Chao; Abudurixiti, Adila; Yusuf, Abdulla

doi:10.1002/slct.202201906

ChemistrySelect

2022

DOI: 10.1002/slct.202201906

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Development and Structural Modifications of Rupestonic Acid Derivatives as Novel Anti‐Influenza Agents: A Mini Review of The Last 10 Years

Abulimiti Yumaier

Zhi‐Chao Cui

Adila Abudurixiti

et al.

Abstract: Artemisia rupestris L. is one of the therapeutic choices to cure influenza and concomitant infections in China. Rupestonic acid is the main active ingredient of this herbal remedy and has activity against the influenza virus. To find a potential lead compound, more than 300 rupestonic derivatives have been synthesized and assayed in vitro against influenza A and B viruses. This systematic review was therefore aimed at summarizing the rupestonic acid derivatives and their anti-influenza activity studied in the … Show more

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2024

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Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity

Yong,

2024

CPD

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Background:: Influenza virus is a kind of RNA virus. Nowadays, the high incidence of influenza and the morbidity and mortality of epidemic influenza are substantial. It has been reported that one hundred million people in the world are infected with influenza viruses, and two hundred and fifty thousand to five hundred thousand people die from the flu per year. In 2021, the number of infected persons in China was reported to be 654,700, and 0.07% of the infected persons died. The flu has caused a serious threat to human survival. Although several drugs, such as Zanamivir, Oseltamivir, Peramivir, and Laninamivir, have been used in clinics for the treatment of the influenza virus, there are some shortcomings of these drugs. The strain of influenza H5N1 (avian influenza) has been found to resist the effective drug Oseltamivir. Thus, there is an urgent demand to discover new anti-influenza virus inhibitors to overcome the emergence of influenza antigens. Aims: This study aimed to develop new anti-influenza virus inhibitors based on the rupestonic acid parent core. Objective:: The rupestonic acid L-ephedrine ester (A) and rupestonic acid L-ephedrine complex (B) were synthesized in this work for the development of anti-influenza virus inhibitors. Methods:: The target compounds were synthesized using rupestonic acid and L-ephedrine as starting materials. Their structures were characterized by 1H NMR and 13C NMR, and the purity was determined by HPLC. Then, their preliminary in vitro anti-influenza activity was evaluated using Oseltamivir as a reference drug. Results:: The results showed that the synthesized rupestonic acid L-ephedrine derivatives A and B were more potent anti-influenza virus agents against the strains of A/PR/8/34 (H1N1) and A/FM/1/47 (H1N1) with the IC50 values of 51.0, 51.0 μM and 441.0, 441.0 μM, respectively, than that of rupestonic acid. By comparing the IC50 of compounds A and B, compound A can be regarded as a very promising lead compound for the development of anti-influenza inhibitors. Conclusion:: The rupestonic acid L-ephedrine ester (A) and rupestonic acid L-ephedrine complex (B) were synthesized and characterized using 1H NMR and 13C NMR. Moreover, their purity was determined by HPLC. Both compounds A and B exhibited more potent activities against the strains of A/PR/8/34 (H1N1) and A/FM/1/47 (H1N1) than rupestonic acid. Compound A can be regarded as a very promising lead compound for the development of anti-influenza inhibitors. Based on these results, more rupestonic acid derivatives will be designed and synthesized in the future for the development of anti-influenza inhibitors.

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Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity

Yong,

2024

CPD

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Development and Structural Modifications of Rupestonic Acid Derivatives as Novel Anti‐Influenza Agents: A Mini Review of The Last 10 Years

Cited by 1 publication

References 20 publications

Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity

Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity

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