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KMID : 0043320220450040280
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Archives of Pharmacal Research
2022 Volume.45 No. 4 p.280 ~ p.293
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Discovery and synthesis of 1,2,4-oxadiazole derivatives as novel inhibitors of Zika, dengue, Japanese encephalitis, and classical swine fever virus infections
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Nam Sang-Woo
Na Hyo-Gyeong
Oh Eun-Hye
Jung Eun-Hye
Lee Yeon-Hee
Jeong Eun-Ju
Ou Yu-Da
Zhou Bin
Ahn Sun-Joo
Shin Jin-Soo
Han Soo-Bong
Go Yun-Young
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Abstract
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Zika virus (ZIKV), an arbovirus of the Flaviviridae family, has emerged as a significant public health concern owing to its association with congenital abnormalities and severe neurological sequelae. Thus, there is an urgent need to develop effective therapeutic approaches to efficiently treat ZIKV infections. This study used phenotypic screening to identify a series of 1,2,4-oxadiazole derivatives that possess antiviral activity against ZIKV infection. Subsequently, 28 new derivatives were designed, synthesized, and evaluated for this purpose. Among these compounds, 4-(5-phenyl-1,2,4-oxadiazol-3-yl)-N-(pyridin-3-ylmethyl)aniline (5d) had potent antiviral activity against ZIKV infections. Furthermore, a structure?activity relationship analysis indicated that a benzyl substitution on the aniline nitrogen of this compound improved potency while augmenting its drug-like properties. In addition, 5d exhibited antiviral activity against various viruses of Flaviviridae family of worldwide public health importance, such as dengue, Japanese encephalitis and classical swine fever viruses, indicating its potential as a lead compound for generating 1,2,4-oxadiazole derivatives with broad-spectrum anti-flaviviral properties.
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KEYWORD
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Antiviral activity, 1,2,4-Oxadiazole derivatives, Zika virus, Dengue virus, Japanese encephalitis virus, Classical swine fever virus
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