Synthesis and Antiviral Activity of N-Phenylbenzamide Derivatives, a Novel Class of Enterovirus 71 Inhibitors

doi:10.3390/molecules18033630

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Molecules 2013, 18(3), 3630-3640; doi:10.3390/molecules18033630

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Synthesis and Antiviral Activity of N-Phenylbenzamide Derivatives, a Novel Class of Enterovirus 71 Inhibitors

Xing-Yue Ji^†, Hui-Qiang Wang^†, Lan-Hu Hao, Wei-Ying He, Rong-Mei Gao, Yan-Ping Li* , Yu-Huan Li* , Jian-Dong Jiang and Zhuo-Rong Li

Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China ^† These authors contributed equally to this work.

* Authors to whom correspondence should be addressed.

Received: 6 January 2013; in revised form: 14 March 2013 / Accepted: 18 March 2013 / Published: 21 March 2013

(This article belongs to the Section Medicinal Chemistry)

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Abstract: A series of novel N-phenylbenzamide derivatives were synthesized and their anti-EV 71 activities were assayed in vitro. Among the compounds tested, 3-amino-N-(4-bromophenyl)-4-methoxybenzamide (1e) was active against the EV 71 strains tested at low micromolar concentrations, with IC₅₀ values ranging from 5.7 ± 0.8–12 ± 1.2 μM, and its cytotoxicity to Vero cells (TC₅₀ = 620 ± 0.0 μM) was far lower than that of pirodavir (TC₅₀ = 31 ± 2.2 μM). Based on these results, compound 1e is a promising lead compound for the development of anti-EV 71 drugs.

Keywords: synthesis; EV 71; N-phenylbenzamide

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Cite This Article

MDPI and ACS Style

Ji, X.-Y.; Wang, H.-Q.; Hao, L.-H.; He, W.-Y.; Gao, R.-M.; Li, Y.-P.; Li, Y.-H.; Jiang, J.-D.; Li, Z.-R. Synthesis and Antiviral Activity of N-Phenylbenzamide Derivatives, a Novel Class of Enterovirus 71 Inhibitors. Molecules 2013, 18, 3630-3640.

AMA Style

Ji X-Y, Wang H-Q, Hao L-H, He W-Y, Gao R-M, Li Y-P, Li Y-H, Jiang J-D, Li Z-R. Synthesis and Antiviral Activity of N-Phenylbenzamide Derivatives, a Novel Class of Enterovirus 71 Inhibitors. Molecules. 2013; 18(3):3630-3640.

Chicago/Turabian Style

Ji, Xing-Yue; Wang, Hui-Qiang; Hao, Lan-Hu; He, Wei-Ying; Gao, Rong-Mei; Li, Yan-Ping; Li, Yu-Huan; Jiang, Jian-Dong; Li, Zhuo-Rong. 2013. "Synthesis and Antiviral Activity of N-Phenylbenzamide Derivatives, a Novel Class of Enterovirus 71 Inhibitors." Molecules 18, no. 3: 3630-3640.

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