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

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

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

Xiao Lu,Yanli Chen,Ying Guo,Zhenming Liu,Yawei Shi,Yang Xu,Xiaowei Wang,Zhili Zhang,Junyi Liu,Xiao Lu,Yanli Chen,Ying Guo,Zhenming Liu,Yawei Shi,Yang Xu,Xiaowei Wang,Zhili Zhang,Junyi Liu,Xiao Lu,Yanli Chen,Ying Guo,Zhenming Liu,Yawei Shi,Yang Xu,Xiaowei Wang,Zhili Zhang,Junyi Liu,

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 IC(50) values (IC(50) 0.82-5.09muM) comparable to that of nevirapine (IC(50) 10.60muM). The biological testing results are in accordance with the docking.

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

X Lu,Y Chen,Y Guo,Z Liu,Y Shi,Y Xu,X Wang,Z Zhang,J Liu,X Lu,Y Chen,Y Guo,Z Liu,Y Shi,Y Xu,X Wang,Z Zhang,J Liu,X Lu,Y Chen,Y Guo,Z Liu,Y Shi,Y Xu,X Wang,Z Zhang,J Liu,

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

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 7399-407

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 28

MONTH: 08

YEAR: 2007

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

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LANGUAGE: eng

NlmUniqueID: 9413298

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

AFFILIATION: Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.

Country: England

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MEDLINETA: Bioorg Med Chem

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