Discovery and optimization of 2, 4-diaminoquinazoline derivatives as a new class of potent dengue virus inhibitors

…, AH Gao, L Yang, J Li, FJ Nan, M Jacobs…

Index: Chao, Bo; Tong, Xian-Kun; Tang, Wei; Li, De-Wen; He, Pei-Lan; Garcia, Jean-Michel; Zeng, Li-Min; Gao, An-Hui; Yang, Li; Li, Jia; Nan, Fa-Jun; Jacobs, Michael; Altmeyer, Ralf; Zuo, Jian-Ping; Hu, You-Hong Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3135 - 3143

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Citation Number: 12

Abstract

The results of a high-throughput screening assay using the DENV-2 replicon showed that the 2, 4-diaminoquinazoline derivative 4a has a high dengue virus inhibitory activity (EC50= 0.15 μM). A series of 2, 4-diaminoquinazoline derivatives based on 4a as a lead compound were synthesized and subjected to structure–antidengue activity relationship studies. Among the series of 2, 4-diaminoquinazoline derivative probed, 4o was observed to ...

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