Synthesis of esters and amides of 2-aryl-1-hydroxy-4-methyl-1H-imidazole-5-carboxylic acids and study of their antiviral activity against orthopoxviruses

Nikitina, Polina A.; Basanova, Elizaveta I.; Николаенкова, Елена Б.; Os’kina, I. A.; Серова, О. А.; Бормотов, Н. И.; Шишкина, Л. Н.; Перевалов, В. П.; Tikhonov, А. Ya.

doi:10.1016/j.bmcl.2022.129080

Cited by 9 publications

(3 citation statements)

References 58 publications

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“…[1] The biological activity of some of the bioactive compounds such as 2-pentanone, and 4-hydroxy-4-methyl have been well reported in the literature. [32,33] The results of the anticancer studies are also in agreement with the cytotoxicity properties of four wild edible mushrooms; Coprinus comatus (O.F. Mull.)…”

Section: Discussionsupporting

confidence: 67%

Comparative Study on Biological Activities and Chemical Profiling of Mushroom (Pleurotus pulmonarius (Fr.) Quel.) Cultured on Lignocellulosic Agro Wastes

Zamakshshari

Ahmed

Nasharuddin

et al. 2023

Chemistry & Biodiversity

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The relevance of the lignocellulosic substrate in the cultivation of mushrooms has lent support to the exploration of several lignocellulosic agro wastes. This study was, thus, aimed at the evaluation of durian peel as an alternative substrate for more sustainable mushroom cultivation and climate change mitigation. The secondary metabolites and biological activities of both aqueous and organic mushroom (Pleurotus pulmonarius (Fr.) Quel.) extract cultured on durian peel and rubberwood sawdust substrate were compared using GCMS, LCMS as well as various biological assays (cytotoxicity, antimicrobial and antioxidant activities). Mushroom extracts from durian peel substrates possess remarkable biological activities. The results showed that the aqueous extracts had poor antimicrobial activities. The organic extracts were more active against cancer cells than the aqueous extracts, while the aqueous extracts were more potent as antioxidants than the organic extracts. Overall, the mushroom extract from the durian substrate was the most effective except against A549 and SW948, while the aqueous extract from the durian substrate was the most effective against the A549 cancer cell lines with 29.53±2.39 % inhibition. On the other hand, the organic mushroom extract from the sawdust substrate was the most effective against SW948 with 60.24±2.45 % inhibition. Further studies, however, are needed to elucidate the molecular mechanism of action of P. pulmonarius extracts against cancer cell proliferation and the effect of the substrates on the nutritional composition, secondary metabolites, and other biological activities of P. pulmonarius extracts.

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Section: Discussionsupporting

confidence: 67%

Comparative Study on Biological Activities and Chemical Profiling of Mushroom (Pleurotus pulmonarius (Fr.) Quel.) Cultured on Lignocellulosic Agro Wastes

Zamakshshari

Ahmed

Nasharuddin

et al. 2023

Chemistry & Biodiversity

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“…A library of 2-aryl-1-hydroxyimidazole derivatives containing ester or carboxamide moieties was synthesized and tested against VACV. 175 The most potent hits 166 and 167 had broad-spectrum antiviral activity against VACV, CPXV, and ECTV. Their antiviral activity appears specific to orthopoxvirus, as they did not show activity against the influenza virus.…”

Section: Virucidal Compoundsmentioning

confidence: 99%

“…A library of 2-aryl-1-hydroxyimidazole derivatives containing ester or carboxamide moieties was synthesized and tested against VACV . The most potent hits 166 and 167 had broad-spectrum antiviral activity against VACV, CPXV, and ECTV.…”

Section: Antivirals Against Orthopoxvirusesmentioning

confidence: 99%

An Overview of Antivirals against Monkeypox Virus and Other Orthopoxviruses

et al. 2023

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The current monkeypox outbreaks during the COVID-19 pandemic have reignited interest in orthopoxvirus antivirals. Monkeypox belongs to the Orthopoxvirus genus of the Poxviridae family, which also includes the variola virus, vaccinia virus, and cowpox virus. Two orally bioavailable drugs, tecovirimat and brincidofovir, have been approved for treating smallpox infections. Given their human safety profiles and in vivo antiviral efficacy in animal models, both drugs have also been recommended to treat monkeypox infection. To facilitate the development of additional orthopoxvirus antivirals, we summarize the antiviral activity, mechanism of action, and mechanism of resistance of orthopoxvirus antivirals. This perspective covers both direct-acting and host-targeting antivirals with an emphasis on drug candidates showing in vivo antiviral efficacy in animal models. We hope to speed the orthopoxvirus antiviral drug discovery by providing medicinal chemists with insights into prioritizing proper drug targets and hits for further development.

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