Bing-Lei Gao

Shandong University, Chi-nan-shih, Shandong Sheng, China

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Publications (3)5.84 Total impact

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    ABSTRACT: A series of new HIV-1 protease inhibitors with the hydroxyethylamine core and different hydroxyprolinamide P2 ligands were designed and synthesized. Variation of substitutions at the P2 significantly affected the enzyme inhibitory potency of the inhibitors. Compounds 2a and 2d showed excellent enzyme inhibitory activity with IC(50) values in the nanomolar range. An active site binding model for inhibitors 2a and 2d was suggested based upon the computational-docking results of the ligand with HIV-1 protease. This model offers molecular insights regarding ligand-binding site interactions of the hydroxyprolinamide-derived novel P2-ligand.
    Bioorganic & medicinal chemistry letters 06/2011; 21(12):3730-3. DOI:10.1016/j.bmcl.2011.04.070 · 2.65 Impact Factor
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    ABSTRACT: A novel simple three-step synthesis of 3-arylated 5,6-dimethoxybenzo[d]isothiazole 1,1-dioxide is reported. ortho-Lithiation of N-tert-butyl-3,4-dimethoxybenzenesulfonamide followed by reaction with aryl aldehydes gave carbinol sulfonamides, which were oxidized into ketosulfonamides and converted to the ketimines via TMSCl/NaI/MeCN reagent mediated novel cyclization.
    Letters in Organic Chemistry 05/2010; 7(4):332-334. DOI:10.2174/157017810791130568 · 0.65 Impact Factor
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    ABSTRACT: In the past twenty years, the development of efficient methods for asymmetric fluorination is one of the most fascinating aspects of modern organofluorine chemistry. Among the many approaches towards the construction of chiral organofluorine compounds containing a fluorine atom bonded directly to a stereogenic center, electrophilic asymmetric fluorination has proven to be particularly effective. In this review, substrate-mediated diastereoselective electrophilic fluorinations for the synthesis of chiral organofluorine compounds is first discussed, followed by chiral reagent-controlled stoichiometric asymmetric electrophilc fluorination of achiral compounds, with emphasis on the developments and applications of neutral chiral N-F agents based on the sultam templates and charged chiral [N-F]+ reagents derived from the fluorinated cinchona alkaloids or the alkaloids/Selectfluor combination.
    Current Organic Chemistry 04/2010; 14(9):889-916. DOI:10.2174/138527210791111812 · 2.54 Impact Factor