1415000-10-0Relevant articles and documents
Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity
Guo, Di-Liang,Zhang, Xing-Jie,Wang, Rui-Rui,Zhou, Yu,Li, Zeng,Xu, Jin-Yi,Chen, Kai-Xian,Zheng, Yong-Tang,Liu, Hong
, p. 7114 - 7118 (2013/01/15)
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 3a could meet the HIV-1 integrase inhibition minimal requirements of a chelating domain (two metal ions) and an aromatic domain (π-π stacking interactions).