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 Научная публикация
| Журнал |
Bioorganic and Medicinal Chemistry Letters
ISSN: 0960-894X , E-ISSN: 1464-3405 |
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| Вых. Данные | Год: 2023, Том: 79, Страницы: 129080 Страниц : 1 DOI: 10.1016/j.bmcl.2022.129080 | ||||||
| Ключевые слова | 1-Hydroxyimidazole, Vaccinia virus, Antiviral activity, Cytotoxicity, Orthopoxviruses | ||||||
| Авторы |
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Реферат:
Smallpox was eradicated >40 years ago but it is not a reason to forget forever about orthopoxviruses pathogenic
to humans. Though in 1980 the decision of WHO to cease vaccination against smallpox had seemed logical, it led
to the decrease of cross immunity against other infections caused by orthopoxviruses. As a result, in 2022 the
multi-country monkeypox outbreak becomes a topic of great concern. In spite of existing FDA-approved drugs for
the treatment of such diseases, the search for new small-molecule orthopoxvirus inhibitors continues. In the
course of this search a series of novel 2-aryl-1-hydroxyimidazole derivatives containing ester or carboxamide
moieties in position 5 of heterocycle has been synthesized and tested for activity against Vaccinia virus in Vero
cell culture. Some of the compounds under consideration revealed a selectivity index higher than that of the
reference drug Cidofovir. The highest selectivity index SI = 919 was exhibited by ethyl 1-hydroxy-4-methyl-2-[4-
(trifluoromethyl)phenyl]-1H-imidazole-5-carboxylate 1f. The most active compound also demonstrated inhibitory activity against the cowpox virus (SI = 20) and the ectromelia virus (SI = 46).
Библиографическая ссылка:
Nikitina P.A.
, Basanova E.I.
, Nikolaenkova E.B.
, Os'kina I.A.
, Serova O.A.
, Bormotov N.I.
, Shishkina L.N.
, Perevalov V.P.
, Tikhonov A.Y.
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
Bioorganic and Medicinal Chemistry Letters. 2023. V.79. P.129080. DOI: 10.1016/j.bmcl.2022.129080 WOS РИНЦ OpenAlex
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
Bioorganic and Medicinal Chemistry Letters. 2023. V.79. P.129080. DOI: 10.1016/j.bmcl.2022.129080 WOS РИНЦ OpenAlex
Даты:
| Поступила в редакцию: | 13 окт. 2022 г. |
| Принята к публикации: | 16 нояб. 2022 г. |
| Опубликована online: | 19 нояб. 2022 г. |
Идентификаторы БД:
| Web of science: | WOS:000904529600004 |
| РИНЦ: | 54610071 |
| OpenAlex: | W4309580618 |