38711-03-4Relevant academic research and scientific papers
Discovery and optimization of 2,4-diaminoquinazoline derivatives as a new class of potent dengue virus inhibitors
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
, p. 3135 - 3143 (2012/06/01)
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 display both the highest antiviral potency (EC50 = 2.8 nM, SI > 1000) and an excellent pharmacokinetic profile.
