957148-83-3Relevant academic research and scientific papers
The design and synthesis of N-1-alkylated-5-aminoaryalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors
Lu, Xiao,Chen, Yanli,Guo, Ying,Liu, Zhenming,Shi, Yawei,Xu, Yang,Wang, Xiaowei,Zhang, Zhili,Liu, Junyi
, p. 7399 - 7407 (2007)
Novel compounds 1a-u, which can be considered as hybrid analogues of MKC-442 and pyridinon, have been synthesized and evaluated as inhibitors of HIV-1 reverse transcriptase (HIV-1 RT). Starting from 6-methyuracil 2, 1-alkylated-5-bromomethyl-6-methyluracils 8 was prepared in four steps by hydroxylmethylation, etherification, N-1 alkylation, and bromination. Finally, compounds 1a-u were achieved in the displacement of 5-bromomethyl group by nucleophiles with amino compounds. Some of compounds 1a-u showed potent inhibitory activity against HIV-1 RT. The most active compounds showed activity in the low micromolecular range with IC50 values (IC50 0.82-5.09 μM) comparable to that of nevirapine (IC50 10.60 μM). The biological testing results are in accordance with the docking.
