Synthesis and in vitro antiviral evaluation of 4-substituted 3,4-dihydropyrimidinones

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• 作者：Dhanabal Kumarasamy^a ; ^{dhanabalrx@gmail.com} ; Biswajit Gopal Roy^b ; Joana Rocha-Pereira^c ; Johan Neyts^c ; Satheeshkumar Nanjappan^d ; Subhasis Maity^a ; Musfiqua Mookerjee^a ; Lieve Naesens^c
• 关键词：Dihydropyrimidinones ; DHPM ; Antiviral activity ; Cytotoxicity ; Bunyavirus
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：27
• 期：2
• 页码：139-142
• 全文大小：481 K
• 卷排序：27

文摘

A series of 4-substituted 3,4-dihydropyrimidine-2-ones (DHPM) was synthesized, characterized by IR, 1H NMR, 13C NMR and HRMS spectra. The compounds were evaluated in vitro for their antiviral activity against a broad range of DNA and RNA viruses, along with assessment for potential cytotoxicity in diverse mammalian cell lines. Compound 4m, which possesses a long lipophilic side chain, was found to be a potent and selective inhibitor of Punta Toro virus, a member of the Bunyaviridae. For Rift Valley fever virus, which is another Bunyavirus, the activity of 4m was negligible. DHPMs with a C-4 aryl moiety bearing halogen substitution (4b, 4c and 4d) were found to be cytotoxic in MT4 cells.