The design and synthesis of N-1-alkylated-5-aminoaryalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors

X Lu, Y Chen, Y Guo, Z Liu, Y Shi, Y Xu, X Wang…

Index: Lu, Xiao; Chen, Yanli; Guo, Ying; Liu, Zhenming; Shi, Yawei; Xu, Yang; Wang, Xiaowei; Zhang, Zhili; Liu, Junyi Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 23 p. 7399 - 7407

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Citation Number: 36

Abstract

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- ...