Structural modifications of 5, 6-dihydroxypyrimidines with anti-HIV activity

…, Y Zhou, Z Li, JY Xu, KX Chen, YT Zheng, H Liu

Index: Guo, Di-Liang; Zhang, Xing-Jie; Wang, Rui-Rui; Zhou, Yu; Li, Zeng; Xu, Jin-Yi; Chen, Kai-Xian; Zheng, Yong-Tang; Liu, Hong Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7114 - 7118

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Citation Number: 2

Abstract

A series of 5, 6-dihydroxypyrimidine analogs were synthesized and evaluated for their anti- HIV activity in vitro. Among all of the analogs, several compounds exhibited significant anti- HIV activity, especially 1b and 1e, which showed the most potent anti-HIV activity with EC50 values of 0.14 and 0.15 μM, and TI (therapeutic index) values of> 300 and> 900, respectively. Further docking studies revealed that the representative compounds 1e and ...