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Issue 4, 2016
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A stereo configuration-activity study of 3-iodo-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(2H)-ones as potency inhibitors of HIV-1 variants

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Abstract

3-Iodo-4-(2′-methylcyclohexyloxy)-6-phenethylpyridin-2(1H)-ones, as effective non-nucleoside reverse transcriptase inhibitors, were synthesized and resolved with different configurations. Biological results revealed that the trans-racemate 2b exhibited more potent activity than the cis-isomers. Noticeably, the trans-(S,S)-enantiomer 2e turned out to be significantly more potent than its counterpart enantiomer 2d against wild-type and double-mutant strains with high selectivity indexes.

Graphical abstract: A stereo configuration-activity study of 3-iodo-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(2H)-ones as potency inhibitors of HIV-1 variants

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Publication details

The article was received on 19 Oct 2015, accepted on 27 Nov 2015 and first published on 08 Dec 2015


Article type: Paper
DOI: 10.1039/C5OB02154E
Org. Biomol. Chem., 2016,14, 1413-1420

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    A stereo configuration-activity study of 3-iodo-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(2H)-ones as potency inhibitors of HIV-1 variants

    S. Wu, Q. Yin, L. Zhao, N. Fan, X. Tang, J. Zhao, T. Sheng, Y. Guo, C. Tian, Z. Zhang, W. Xu, Z. Liu, S. Jiang, L. Ma, J. Liu and X. Wang, Org. Biomol. Chem., 2016, 14, 1413
    DOI: 10.1039/C5OB02154E

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